U.S. patent application number 12/401390 was filed with the patent office on 2009-09-17 for mixtures with a collagen synthesis boosting action.
This patent application is currently assigned to SYMRISE GmbH & Co., KG. Invention is credited to Helge Franke, Sabine Lange, Gerhard Schmaus.
Application Number | 20090232915 12/401390 |
Document ID | / |
Family ID | 41063305 |
Filed Date | 2009-09-17 |
United States Patent
Application |
20090232915 |
Kind Code |
A1 |
Schmaus; Gerhard ; et
al. |
September 17, 2009 |
MIXTURES WITH A COLLAGEN SYNTHESIS BOOSTING ACTION
Abstract
The invention relates to synergistically active, ternary
mixtures which boost collagen synthesis and to the uses thereof, in
particular for slowing down skin ageing and for wound healing of
damaged skin. The invention furthermore relates to the use of the
ternary mixtures according to the invention for treating the oral
cavity and pharynx, and in particular therein for preventing and
slowing down periodontitis, for building up periodontal connective
tissue and for preventing and treating infections in the oral
cavity and for wound healing in the oral cavity.
Inventors: |
Schmaus; Gerhard;
(Hoxter-Bosseborn, DE) ; Franke; Helge; (Dieburg,
DE) ; Lange; Sabine; (Holzminden, DE) |
Correspondence
Address: |
CONNOLLY BOVE LODGE & HUTZ LLP
1875 EYE STREET, N.W., SUITE 1100
WASHINGTON
DC
20006
US
|
Assignee: |
SYMRISE GmbH & Co., KG
Holzminden
DE
|
Family ID: |
41063305 |
Appl. No.: |
12/401390 |
Filed: |
March 10, 2009 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
|
|
61036622 |
Mar 14, 2008 |
|
|
|
Current U.S.
Class: |
424/744 |
Current CPC
Class: |
A61K 8/676 20130101;
A61Q 19/08 20130101; A61K 8/9794 20170801; A61K 8/9789 20170801;
A61K 2800/70 20130101 |
Class at
Publication: |
424/744 |
International
Class: |
A61K 8/97 20060101
A61K008/97; A61Q 19/08 20060101 A61Q019/08 |
Claims
1. A ternary mixture containing, substantially consisting of or
consisting of a) an extract of Aloe plant material, b) ascorbic
acid and/or the derivative(s) thereof, preferably at least one
solvate and/or salt of ascorbic acid and/or at least one ascorbic
acid prodrug, and c) an extract of rosaceous plant material, except
for an aftersun balm simultaneously containing 3.0 wt. % of an Aloe
barbadensis leaf extract 10/1 in water, 1.0 wt. % of sodium
ascorbyl phosphate and 0.5 wt. % of maltodextrin Rubus fruticosus
leaf extract, in each case relative to the entire balsam.
2. The mixture as claimed in claim 1, containing a) an extract of
Aloe plant material, b) sodium and/or magnesium ascorbyl phosphate,
and c) an extract selected from the group consisting of blackberry
leaf extract, raspberry leaf extract, strawberry leaf extract and
meadowsweet herb extract, or two or more such extracts.
3. The mixture as claimed in claim 1 or claim 2, wherein the
proportions of the components in each case amount to: component a):
33-99 wt. %, preferably 80-98 wt. % and particularly preferably
89-96.51 wt. %; component b): 0.99-32.99 wt. %, preferably 1.9-15
wt. % and particularly preferably 3.22-9 wt. %; component c):
0.01-10 wt. %, preferably 0.1-4 wt. % and particularly preferably
0.27-2 wt. %; in each case relative to the total of components a),
b) and c).
4. The mixture as claimed in claims 1, 2 or 3, wherein the
proportions the component in each case amount to: component a):
85-92 wt. %, preferably 88-92 wt. %, particularly preferably 90 wt.
%, component b): 7-10 wt. %, preferably 9 wt. %, component c):
0.5-2 wt. %, preferably 0.8-1.2 wt. %, particularly preferably 1
wt. %, in each case relative to the total of components a), b) and
c), with component b) consisting of magnesium ascorbyl phosphate
and component c) of raspberry leaf extract.
5. A cosmetic, pharmaceutical and/or oral hygiene preparation,
containing a mixture as claimed in any one of claims 1, 2, 3 or 4,
wherein the concentration of the mixture amounts to 0.001-20 wt. %,
preferably 0.01-10 wt. % and particularly preferably amounts to
0.1-5 wt. %, relative to the entire preparation.
6. A cosmetic, pharmaceutical and/or oral hygiene preparation as
claimed in claim 5, containing the mixture as claimed in any one of
claims 1, 2, 3 or 4 in a concentration sufficient for stimulating
collagen synthesis and/or for slowing down skin ageing and/or for
preventing and/or slowing down periodontitis and/or caries.
7. A method for manufacturing a pulverulent mixture as claimed in
claims 1, 2, 3 or 4, comprising mixing components a), b) and c) in
their respective selected amounts to obtain a homogeneous
pulverulent mixture.
8. A method for manufacturing a liquid mixture as claimed in claims
1, 2, 3 or 4, comprising (i) mixing components a), b) and c) in
their respective selected amounts to obtain a, preferably
homogeneous, pulveruient mixture, and subsequently (ii) dissolving
the resultant pulverulent mixture in a medium containing water
and/or an alcohol selected from the group consisting of methanol,
ethanol, n-propanol, isopropanol, and/or an aliphatic polyol
selected from the group consisting of glycerin, propylene glycol,
butylene glycol, 1,2-alkanediols having 3-10 carbon atoms.
9. Use of a mixture as claimed in any one of claims 1, 2, 3 or 4 or
of a cosmetic, pharmaceutical and/or oral hygiene preparation as
claimed in claim 5 or claim 6 for stimulating collagen synthesis in
non-therapeutic manner and/or for slowing down skin ageing in
non-therapeutic manner and/or for preventing and/or slowing down
periodontitis and/or caries in non-therapeutic manner.
Description
[0001] The invention relates to the field of synergistically
active, ternary mixtures which boost collagen synthesis and to the
uses thereof in particular for cosmetic, oral hygiene and
pharmaceutical purposes. Specifically, the invention relates to the
production of ternary mixtures containing (a) at least one extract
of Aloe and (b) at least one substance selected from the group
ascorbic acid and the derivatives thereof and (c) at least one
extract of a rosaceous plant (Rosaceae, rose family), preferably
raspberry leaf extract, strawberry leaf extract, blackberry leaf
extract or meadowsweet herb extract. The invention furthermore
relates to the use of the ternary mixtures for stimulating collagen
synthesis, in particular for the purpose of slowing down skin
ageing, for reducing wrinkle formation, for treating inflammatory
processes of the skin and for wound healing of damaged skin. The
invention furthermore relates to the use of the ternary mixtures
according to the invention for treating the oral cavity and
pharynx, in particular for preventing and slowing down
periodontitis and for building up periodontal connective tissue and
moreover for preventing and treating infections in the oral cavity
and for wound healing in the oral cavity.
[0002] Ageing of human skin is accompanied by increasing wrinkle
formation and declining elasticity and strength. In the context of
the ageing process, a distinction is drawn between intrinsic and
extrinsic skin ageing. Intrinsic ageing encompasses the natural,
genetically determined changes in the skin. Extrinsic skin ageing
describes premature ageing processes which are brought about by
exogenous influences such as sunlight, environmental poisons (e.g.
ozone, tobacco smoke etc.), psychological stress and chronic
inflammation. Ultraviolet radiation is the most significant
exogenous noxious agent to cause premature ageing of human skin
(photoageing). In addition to natural sunlight, irradiation of the
human skin with artificial UV radiation (solarium) is becoming ever
more significant.
[0003] The structural changes responsible for the clinical picture
of aged skin primarily take place in the dermis. The elasticity and
strength of skin are substantially determined by the two main
constituents of the dermal extracellular matrix, the two fibrous
proteins collagen and elastin. The dermis mainly contains collagen
1 (90-85%), which is formed exclusively by dermal fibroblasts, and
significantly smaller amounts (10-15%) of collagen 3. Elastin, the
main constituent of the elastic fibers of the skin in addition to
fibrillin, is present in the dermis in an amount of approx.
1-3%.
[0004] In comparison with young skin, old skin is characterized by
a declining concentration of collagen and elastin. This age-related
tissue loss is brought about by the reduction in de novo collagen
synthesis which accompanies ageing and by an imbalance between the
activation and inhibition of proteolytic activity, which is
accompanied by increased degradation of collagen.
[0005] Offsetting the effects brought about by intrinsic and
extrinsic skin ageing such as reduced de novo collagen synthesis
and increased proteolytic activity by MMPs, in particular MMP-1,
-2, -3 and -9, is thus an important goal in the development of new
cosmetic active ingredients to counter skin ageing and
wrinkles.
[0006] Retaining an elevated collagen content in the skin or
increasing the collagen content in the skin may be achieved in
various different ways. On the one hand, substances which inhibit
matrix metalloproteinases may be used. On the other hand, however,
it is also possible to use substances which increase collagen
synthesis in order, by de novo synthesis, to counter the negative
effects of MMP-induced collagen degradation. The reduction in de
novo collagen synthesis which accompanies increasing age may here
be at least partially compensated by using active ingredients which
increase collagen synthesis.
[0007] Individual substances which are frequently mentioned in
connection with increasing collagen synthesis and are thus prior
art are for example active ingredients such as ascorbic acid and
the derivatives thereof, retinol and derivatives of retinol or
plant extracts such as for example extracts of Aloe and Centella
species. Active ingredients which are furthermore frequently used
to boost collagen synthesis also include peptide substances and the
derivatives thereof such as e.g. carnitine, carnosine, creatine,
matrikine peptides (e.g. lysyl-threonyl-threonyl-lysyl-serine) and
further peptide structures such as palmitoylated pentapeptides
(e.g. Matrixyl from Sederma) or the oligopeptide with the trade
name Vincipeptide (from Vincience, France). Moreover, compounds
such as asiatic acid, madecassic acid, madecassoside, asiaticoside,
extracts of Centella asiatica, niacinamide, astaxanthine, glucans
e.g. from yeasts and oats, soy extract and soy isoflavones, such as
genistein and daidzein, rutin, chrysin, morin, betel nut alkaloids,
forskolin, betulinic acid, extracts of Plantago species, TGF-beta,
extracts of Ginkgo biloba, glutamine and glycolic acid are used as
collagen synthesis stimulators. In contrast, no mention has been
made of achieving a synergistically enhanced boost in collagen
synthesis by the use of the ternary mixtures according to the
invention.
[0008] Matrix metalloproteinases, a group of enzymes which are
capable of proteolytically degrading the macromolecules of the
extracellular matrix (ECM), which also include collagen, also play
a significant role in skin ageing. Ultimately, this means that MMPs
precisely counteract de novo collagen synthesis. It has accordingly
been established that old skin has a content of MMPs which is
distinctly higher than that of young skin (J. H. Chung et al., J.
Invest. Dermatol, 2001, 117, 1218-1224). MMPs have broad, often
overlapping substrate specificity and, in combination, they are
capable of breaking down all the protein components of the
extracellular matrix. Around 20 MMPs have hitherto been identified.
The are generally secreted as inactive proenzymes (pro-MMP). In
human skin, a major role is played primarily by MMP-1 (collagenase
1), MMP-2 (gelatinase A), MMP-9 (gelatinase B) and MMP-3. Apart
from cleaving collagen 1 and 3, MMP-1 also cleaves pro-MMP-2 and
pro-MMP-9, so activating them. MMP-2 and MMP-9 are among the
elastin-degrading proteases (A. Thibodeau, Cosmetics &
Toiletries 2000, 115 (11), 75-82).
[0009] MMPs also play a decisive role in premature skin aging
brought about by exogenous factors. A still further increased level
of MMPs has been detected in light-aged skin relative to aged skin
provided with light protection (J. H. Chung et al., J. Invest.
Dermatol, 2001, 117, 1218-1224). Induction of matrix
metalloproteinases has been demonstrated not only for UVA and UVB
radiation, but also for infrared radiation. Such induction has been
observed both in vitro in cultured human dermal fibroblasts and in
vivo in UV-irradiated human skin. Stimulation with tobacco smoke
also led in human dermal fibroblasts to upregulation of MMP-1 and
-3 expression (J. Krutmann, Hautarzt 2003, 54, 809-817).
[0010] The use of substances which inhibit MMP-1 (e.g. retinyl
palmitate, propyl gallate, precocene,
6-hydroxy-7-methoxy-2,2-dimethyl-1(2H)-benzopyran,
3,4-dihydro-6-hydroxy-7-methoxy-2,2-dimethyl-1 (2H)-benzopyran) for
preventing sunlight- and/or heat-induced ageing of human skin is
known and has been described e.g. in WO 01/74320.
[0011] It is furthermore known that matrix metalloproteinases are
in particular also of significance in pathological changes in the
oral cavity, e.g. of the periodontium. Periodontitis (also known as
"periodontosis") is an inflammation of the periodontium, i.e. of
the tooth supporting structures. The periodontium comprises various
tissues: the gum epithelium (gingiva), the connective tissue of the
gingiva, the periodontal ligament (desmodontium), the root cement
and the surrounding alveolar bone. The desmodontium is located
between the root surface and the alveolar bone. This is a cell-rich
connective tissue which anchors the tooth in the bony tooth socket,
the alveolus. The desmodontal gap is 53-74% occupied by collagen
and oxytalan fiber bundles. That part of the desmodontal fibers
embedded in the root cement and in the alveolar bone anchors the
tooth in the alveolus. Among the main clinical signs of
periodontitis are inflammation of the gums associated with wound
formation, loss of attachment, formation of periodontal pockets and
alveolar bone breakdown.
[0012] The main cause of periodontitis is plaque. This consists of
certain constituents of the saliva, food residues and, above all,
of bacteria and their breakdown products. This particular type of
infectious disease is in most cases caused by Porphyromonas
gingivalis, Bacteroides forsythus and Actinobacillus
actinomycetemcomitans. Continuous release of bacterial toxins, in
particular of lipopolysaccharides, probably triggers the release of
proinflammatory mediators, such as e.g. IL-1beta, TNF-alpha and
PGE2 in the patients affected tissues. These signaling substances
stimulate the infiltration of immunocompetent cells into the
colonized tissue. Immigration of neutrophilic granulocytes and
macrophages subsequently leads to inflammation of the gums
(gingivitis) and to the release of proinflammatory mediators such
as for example IL-1 and IL-6. These in turn activate the synthesis
in the skin and mucous membranes of matrix-degrading
metalloproteinases (matrix metalloproteinases, MMPs), which break
down the extracellular matrix of the surrounding connective tissue.
As a result, bacteria, which initially interacted with the gingival
line, penetrate deep into the underlying connective tissue, where
they continue inflammatory processes and the synthesis of MMPs and
ultimately detach the uppermost layer of the epithelium from the
dental root. This results in the formation of a periodontal pocket.
The body's response involves inflammation of the gingiva and of the
periodontium accompanied by damage to the alveolar bone. In the
final stage of periodontitis, the sufferer is at risk of massive
tooth loss, furthermore accompanied by infections of the oral
cavity and wound formation.
[0013] Studies (T. Kuboto et al., Arch. Oral. Biol. 1996, 41,
253-262; A. L. Ejeil et al., J. Periodontol. 2003, 74, 188-195)
have shown that the levels of a series of matrix metalloproteinases
(MMP-1, -3, -8, -9 and -13) are significantly increased in patients
with inflammation of the gums in comparison with patients with
healthy gums. These levels correlate with the severity of the
gingivitis or periodontitis. There is furthermore a significant
decrease in collagen fibers as the extent of inflammation of the
gums increases. MMP-9 here clearly acts as a marker in the early
stage of periodontitis (A. L. Ejeil et al., J. Periodontol. 2003,
74, 188-195). Compensating these effects caused by the boost in
collagen synthesis with the assistance of the synergistically
active ternary mixtures is therefore likewise advantageously
indicated.
[0014] MMPs also play an important part in the genesis of caries
and in losses of hard tooth structure, such as for example erosion,
which are not caused by caries. Teeth are mainly composed of a
bone-like substance known as dentine. In the area of the dental
crown which projects out from the gums, the dentine is coated with
a protective layer of dental enamel. Approx. 30% of the dentine
consists of a cell-free matrix primarily containing glycoproteins,
in which are embedded collagen fibers and inorganic
constituents.
[0015] The genesis of caries and erosion accompanies
demineralization of the teeth. Mineral substances are largely
responsible for tooth hardness. The formation of acids by oral
bacteria after consuming sugary foodstuffs, on the one hand, as
well as frequent contact with strongly acidic beverages (e.g. fruit
juices) and strongly acidic foods (tropical fruit, pineapple etc.)
result in demineralization of the dental enamel and, as the process
progresses, also of the dentine. Demineralized dentine is
susceptible to degradation. It has been possible to demonstrate in
vitro that degradation of the organic matrix is necessary for the
formation of a hole in the tooth. Tjaderhane et al. (J. Dent. Res.
1998, 77, 1622-1629) detected MMP-2, MMP-8 and MMP-9 in caries
lesions and established that these are activated by acids. Slowing
down and ideally completely suppressing these effects largely
brought about by collagen degradation with the assistance of the
synergistic active ternary mixtures is therefore likewise
advantageously indicated.
[0016] Pashley et al. (J. Dent. Res. 2004, 83, 216-221) have shown
that, even in the absence of bacteria, collagenolytically active
proteinases cause degradation of collagen fibers of the organic
matrix in dentine which has been partially demineralized by acids.
Degradation of collagen fibers was prevented by addition of
chlorhexidine or protease inhibitors (MMP inhibitor: benzamidine
hydrochloride, cysteine protease inhibitor: N-ethylmaleimide,
epsilon-amino-n-caproic acid, serine protease inhibitor:
phenylmethylsulfonyl fluoride). Slowing down and ideally completely
suppressing these effects largely brought about by collagen
degradation with the assistance of the synergistic active ternary
mixtures is therefore likewise advantageously indicated.
[0017] Maintaining the health or slowing the degradation of the
connective tissue of the periodontium and the collagen fibers of
the teeth, on the one hand, by preventing damage by MMPs by using
matrix metalloproteinase inhibitors and, on the other hand, by
increased formation of collagen by collagen synthesis boosting
active ingredients are therefore important strategies when
developing new active ingredients for oral care or oral hygiene. If
the described processes are to be effectively halted, the damage
caused by MMPs and in this case in particular by MMP-1 (collagenase
1), MMP-2 (gelatinase A), MMP-8 (collagenase 2) and MMP-9
(gelatinase B) must be inhibited at a very early stage.
[0018] Various publications describe the use of synthetic MMP
inhibitors in periodontal disease (M. E. Ryan et al., Curr. Opin.
Periodontal. 1996, 3, 85-96; R. Gendron et al., Clin. Diagn. Lab.
Immunol. 1999, 6, 437-439). Compensating these effects by boosting
the formation of collagen with the assistance of the
synergistically active ternary mixtures is likewise advantageously
indicated, since substances which boost collagen synthesis
counteract by de novo synthesis the negative effects of MMP-induced
collagen degradation.
[0019] It was accordingly the object of the present invention to
provide agents which significantly boost de novo collagen synthesis
relative to the prior art and so contribute to slowing down skin
ageing and to protecting the skin and mucous membranes of the
periodontium and to protecting the organic matrix of the dentine or
counteracting damage to and/or excessive degradation of collagen.
The agents according to the invention should, insofar as use on a
user's skin is desired, where possible be particularly active
against extrinsic skin ageing and the exogenous influencing factors
associated therewith. The agents to be provided should, where
possible, be of natural origin, be easy to manufacture, have good
storage properties and be usable in numerous different
preparations, in particular in cosmetic and pharmaceutical
preparations and in preparations for oral hygiene. It is
furthermore intended to provide production methods for
corresponding agents and uses thereof.
[0020] For the purposes of the invention, an oral hygiene product
(hereinafter also referred to as an oral care product or oral
hygiene preparation) is taken to mean one of the formulations
familiar to a person skilled in the art for cleaning and caring for
the oral and pharyngeal cavity and for freshening the breath. This
expressly includes care of the teeth and gums. Dosage forms of
customary oral hygiene formulations are creams, gels, pastes,
foams, emulsions, suspensions, aerosols, sprays and capsules,
granules, pastilles, tablets, candies or chewing gums, this list
being understood not to be limiting for the purposes of the present
invention.
[0021] The present invention accordingly provides a ternary mixture
containing, substantially consisting of or consisting of
a) an extract of Aloe plant material, b) ascorbic acid and/or the
derivative(s) thereof, preferably at least one solvate and/or salt
of ascorbic acid and/or at least one ascorbic acid prodrug, and c)
an extract of rosaceous plant material, except for an aftersun balm
simultaneously containing 3.0 wt. % of an Aloe barbadensis leaf
extract 10/1 in water, 1.0 wt. % of sodium ascorbyl phosphate and
0.5 wt. % of maltodextrin Rubus fruticosus leaf extract, in each
case relative to the entire balsam.
[0022] Cosmetic and pharmaceutical agents which boost collagen
synthesis are already known as such. Agents which are already
frequently used for this purpose are retinol derivatives such as
retinoic acid, retinal, retinol, retinyl acetate or retinyl
palmitate, ascorbic acid and the derivatives thereof such as in
particular ascorbyl palmitate, magnesium ascorbyl phosphate, sodium
ascorbyl phosphate and ascorbyl alpha- and beta-glucoside. In
addition, a whole series of further active ingredients and plant
extracts are described as stimulators of collagen synthesis:
peptide substances and the derivatives thereof such as e.g.
carnitine, carnosine, creatine, matrikine peptides (e.g.
lysyl-threonyl-threonyl-lysyl-serine) and further peptide
structures such as palmitoylated pentapeptides (e.g. Matrixyl from
Sederma) or the oligopeptide with the trade name Vincipeptide (from
Vincience/France), and substances such as asiatic acid, madecassic
acid, madecassoside, asiaticoside, extracts of Aloe and Centella
species, niacinamide, astaxanthine, glucans e.g. from yeasts and
oats, soy extracts and soy isoflavones, such as genistein and
daidzein and furthermore rutin, chrysin, morin, betel nut
alkaloids, forskolin, betulinic acid, extracts of Plantago species,
TGF-beta, extracts of Ginkgo biloba, glutamine and glycolic acid.
In most cases, however, only little is known about the biological
mechanism of the collagen synthesis boosting effect.
[0023] The use of ternary mixtures containing Aloe extract, at
least one substance selected from the group ascorbic acid and the
derivatives thereof and at least one rosaceous plant extract,
preferably raspberry leaf extract, strawberry leaf extract,
blackberry leaf extract or meadowsweet herb extract for boosting
collagen synthesis has, in contrast, not to date been reported in
the literature.
[0024] Our own investigations have surprisingly shown that in
particular mixtures containing Aloe extract, at least one substance
selected from the group ascorbic acid and the derivatives thereof
and at least one rosaceous plant extract, preferably raspberry leaf
extract, strawberry leaf extract, blackberry leaf extract or
meadowsweet herb extract have excellent collagen synthesis boosting
characteristics. Activity was here synergistically enhanced in
comparison with products consisting solely of Aloe extract, solely
of at least one substance selected from the group ascorbic acid and
the derivatives thereof or solely of at least one rosaceous plant
extract, preferably raspberry leaf extract, strawberry leaf
extract, blackberry leaf extract or meadowsweet herb extract. It
proved possible unambiguously to demonstrate the synergistically
enhanced activity of the ternary mixtures by calculating synergy
index (SI) values with the assistance of Kull's equation
(literature: F. C. Kull et al, Applied Microbiology Vol. 9, p.
538-541 (1961); D. C. Steinberg, Cosmetics & Toiletries Vol.
115(11), 59-62 (2000)).
[0025] A further, unexpected advantage of the mixtures according to
the invention is their slight intrinsic odor, as a result of which
they may particularly advantageously be used in cosmetics and
especially in leave-on products, since the mixtures according to
the invention accordingly bring about scarcely any or absolutely no
changes to the appearance and odor of a cosmetic preparation
containing even high concentrations of the extract. The mixtures
additionally have weak, pleasant intrinsic taste. This additionally
makes the mixtures suitable for use in oral hygiene products,
since, in the case of use in the oral cavity, taste is an important
acceptance criteria for users and is thus ultimately decisive with
regard to the success of using the oral hygiene product.
[0026] The extract of Aloe plant material is particularly
preferably produced from Aloe barbadensis and Aloe vera.
[0027] Preferred ascorbic acid derivatives are: sodium ascorbyl
phosphate, magnesium ascorbyl phosphate, 3-O-ethyl ascorbic acid,
allantoin ascorbate, aminopropyl ascorbyl phosphate, ascorbyl
palmitate, araboascorbic acid monosodium salt, ascorbic acid
polypeptide, ascorbosilane C, ascorbyl dipalmitate, ascorbyl
alpha-glucoside, ascorbyl beta-glucoside, ascorbyl inositol
nicotinate, ascorbyl linoleate, ascorbyl methylsilanol pectinate,
ascorbyl nicotinamide, ascorbyl stearate, ascorbyl
tetraisopalmitate, ascorbyl tocopherol maleate, calcium ascorbate,
chitosan ascorbate, D-arabino-ascorbic acid, disodium ascorbyl
sulfate, glucosamine ascorbate, inositol hexanicotinate
hexaascorbate, isoascorbic acid, L-ascorbic acid, 2-(dihydrogen
phosphate), 2-[3-cholest-5-en-3-yl hydrogen phosphate],
2-O-D-glucopyranosyl-, L-ascorbic acid, 3-O-ethyl ether, magnesium
ascorbate, magnesium ascorbylborate, methoxy PEG-7 ascorbic acid,
methylsilanol ascorbate, potassium ascorbyl tocopheryl phosphate,
potassium ascorbylborate, sodium ascorbate, sodium
ascorbyl/cholesteryl phosphate, sodium isoascorbate, sodium
L-ascorbyl-2-phosphate, tetrahexyldecyl ascorbate, rosaceous plant
extracts are here preferably obtained with a extracting agent
consisting of pure water, pure ethanol or of ethanol/water mixtures
in any desired quantity ratios from 99:1 (99 parts by weight of
ethanol mixed with 1 part by weight of water) to 1:99 (1 part by
weight of ethanol mixed with 99 parts by weight of water). The
extracts are preferably further processed into pulverulent products
by conventional, gentle drying processes such as e.g. spray drying
or vacuum belt drying. Carriers such as e.g. maltodextrin may here
be added in the concentration range from 10% to 95% and preferably
in the concentration range from 30% to 80%.
[0028] All the stated active ingredients may be produced in either
crystalline or powder form. Preferred methods for producing the
ternary mixtures according to the invention are therefore any
methods usual in the cosmetics industry and the pharmaceuticals
industry for producing stable powder mixtures having a homogeneous
distribution. It may, however, furthermore also be advantageous to
produce the ternary mixtures according to the invention in the form
of solutions. Particularly suitable solvents are here water,
monohydric alcohols comprising from 1 to 5 C atoms such as in
particular ethanol, propanol and butanol and polyhydroxylated
aliphatic compounds such as in particular glycerin, propylene
glycol, butylene glycol and 1,2-alkanediols having from 3-10 C
atoms.
[0029] The concentration ratios of the ternary mixtures according
to the invention containing in each case at least one of components
a) to c) may here be selected as desired in the following manner,
the following quantity distributions being preferred according to
the invention:
component a): 0.01 weight percent to 99 weight percent and/or
component b): 0.01 weight percent to 99 weight percent and/or
component c): 0.01 weight percent to 99 weight percent, in each
case relative to the total of components a), b) and c).
[0030] Preferred synergistically active ternary mixtures, on the
other hand, contain an excess of component a), a moderate amount of
component b) and, relative to components a) and b), a small amount
of component c). Preferred mixtures are therefore those in which
the proportions amount to,
component a): 33-99 wt. % component b): 0.99-32.99 wt. % component
c): 0.01-10 wt. %, in each case relative to the total of components
a), b) and c).
[0031] Synergistically boosted collagen synthesis may in particular
be brought about with these quantity ratios.
[0032] Particularly preferred synergistically active ternary
mixtures contain components a) to c) in the following quantity
distribution:
component a): 80 to 98 wt. % component b): 1.9 to 15 wt. %
component c): 0.1 to 4 wt. %
[0033] A very particularly preferred synergistically active ternary
mixture contains components a) to c) in the following quantity
distribution:
component a): 96.51 wt. % component b): 3.22 wt. % component c):
0.27 wt. %, in each case relative to the total of components a), b)
and c).
[0034] The following composition is particularly preferred as a
synergistically active ternary mixture containing raspberry leaf
extract:
component a): 85-92 wt. %, preferably 88-92 wt. %, particularly
preferably 90 wt. %, component b): 7-10 wt. %, preferably 9 wt. %,
component c): 0.5-2 wt. %, preferably 0.8-1.2 wt. %, particularly
preferably 1 wt. %, in each case relative to the total of
components a), b) and c), with component b) consisting of magnesium
ascorbyl phosphate and component c) of raspberry leaf extract.
[0035] A synergistically active ternary mixture which is
particularly preferred in this connection contains components a) to
c) in the following quantity distribution:
component a): 90.00 wt. % component b), namely magnesium ascorbyl
phosphate: 9.00 wt. % component c), namely raspberry leaf extract:
1.00 wt. %, in each case relative to the total of components a), b)
and c).
[0036] The concentration of the ternary mixtures (in liquid and/or
concentrated form) in cosmetic, oral hygiene and/or pharmaceutical
preparations (in particular for topical application) is preferably
in the range from 0.001 to 20 wt. %, preferably in the range from
0.01 to 10 wt. % and particularly preferably in the range from 0.1
to 5 wt. %, relative to the entire preparation. These
concentrations are particularly preferred for synergistically
stimulating collagen synthesis. They are furthermore preferred
[0037] for slowing down skin ageing and/or [0038] for preventing
and/or slowing down periodontitis and/or caries.
[0039] The mixtures according to the invention are preferably
produced according to the invention by a method involving mixing
components a), b) and c) in their respectively selected amounts to
obtain a homogeneous pulverulent mixture.
[0040] The ternary mixtures according to the invention in powder or
liquid form may preferably be further processed to yield a final
product, likewise according to the invention, in preferably liquid
form, by adding to the production method according to the invention
the step: combining the ternary mixture with a further solvent or
carrier which is acceptable for pharmaceutical, oral hygiene and/or
cosmetic purposes.
[0041] The collagen synthesis boosting ternary mixtures according
to the invention are surprisingly ideally suitable as cosmetic
and/or pharmaceutical agents for preventing, alleviating and
treating unwanted changes in the oral cavity which are attributable
to elevated activity of MMPs and the concomitant degradation of
collagen, since they compensate the negative effects of the MMPs by
boosting de novo synthesis of collagen. Combined use of the
collagen synthesis boosting mixtures according to the invention
together MMP inhibitors which are not according to the invention
may here likewise be advantageous.
[0042] For the purposes of the present invention, a carrier which
is acceptable for pharmaceutical, oral hygiene or cosmetic purposes
is a carrier which is at least nontoxic for the organism on which
it is to be used. Preferred solids which are suitable for cosmetic,
oral hygiene or pharmaceutical purposes are pulverulent
maltodextrin, lactose, silicon dioxide or glucose and mixtures of
two or more of these solids. An acceptable solid which is
particularly preferred according to the invention for oral hygiene
purposes is silicon dioxide. Further acceptable solids which may be
used according to the invention for oral hygiene purposes are
hydrocolloids such as starches, degraded starches, chemically or
physically modified starches, modified celluloses, gum arabic, gum
ghatti, tragacanth, karaya, carrageenan, pullulan, curdlan, xanthan
gum, gellan gum, guar flour, locust bean flour, alginates, agar,
pectin and inulin together with mixtures of two or more of these
solids, in particular also with silicon dioxide.
[0043] The solid or liquid ternary mixture may also be further
processed according to the invention to yield a preferably liquid
preparation by [mixing] the ternary mixture with a further solvent
selected from the group consisting of glycerin, 1,2-propylene
glycol, 1,3-butylene glycol, ethanol, water and mixtures of two or
more of the stated solvents with water. Such final products
produced according to the invention may in particular readily be
further processed for cosmetic and oral hygiene purposes. These
preparations according to the invention may optionally be produced
with addition of a preservative, solubilizing agent or antioxidant.
Furthermore, the solid or liquid ternary mixtures according to the
invention or the liquid or solid preparation also according to the
invention containing a solid or liquid ternary mixture according to
the invention may be further processed by encapsulation. According
to the invention, the solid or liquid ternary mixtures according to
the invention or the liquid or solid preparation containing a solid
or liquid ternary mixture according to the invention are
encapsulated with a solid shell material which is preferably
selected from starches, degraded or chemically or physically
modified starches (in particular dextrins and maltodextrins),
gelatins, gum arabic, agar-agar, gum ghatti, gellan gum, modified
and unmodified celluloses, pullulan, curdlan, carrageenans, alginic
acid, alginates, pectin, inulin, xanthan gum and mixtures of two or
more of the stated substances.
[0044] The solid shell material is preferably selected from gelatin
(pig, cattle, chicken and/or fish gelatins and mixtures thereof are
advantageous, preferably comprising at least one gelatin with a
Bloom value of greater than or equal to 200, preferably with a
Bloom value of greater than or equal to 240), maltodextrin
(preferably obtained from maize, wheat, tapioca or potato,
preferred maltodextrins have a DE value in the range from 10-20),
modified cellulose (e.g. cellulose ethers), alginates (e.g. Na
alginate), carrageenan (beta-, iota-, lambda- and/or
kappa-carrageenan), gum arabic, curdlan and/or agar-agar. Gelatin
is in particular preferably used thanks to its readily availability
in different Bloom values. In particular, seamless gelatin or
alginate capsules, the shell of which dissolves very quickly in the
mouth or bursts when chewed and so releases the active ingredient
into the oral cavity are particularly preferably used for oral
hygiene purposes. Production may proceed, for example, as described
in EP 0 389 700, JP 7 196 478, U.S. Pat. No. 4,251,195, U.S. Pat.
No. 6,214,376, WO 03/055587 or WO 2004/050069.
[0045] The synergistically active ternary mixture containing at
least one extract of an Aloe species selected from a), at least one
substance from the group of ascorbic acid and the derivatives
thereof selected from b) and at least one rosaceous plant extract,
preferably raspberry leaf extract, strawberry leaf extract,
blackberry leaf extract or meadowsweet herb extract selected from
c) may advantageously be used in cosmetics in any applications in
which a boost in collagen synthesis is associated with cosmetically
desired effects. Preferably, however, the mixture is used as an
active ingredient against natural and premature, for example
sunlight-induced, skin ageing and against wrinkles. To this end, it
is preferably applied topically onto the skin to be treated.
[0046] Substantial areas of application are here cosmetic, in
particular dermatological preparations, which (apart from
components a)-c) according to the invention) are of conventional
composition and cosmetic, in particular dermatological
photoprotection, for the treatment, care and cleaning of skin
and/or hair or as a makeup product in decorative cosmetics.
Depending on their composition, such preparations may accordingly
for example be used as a skin protection cream, day or night cream,
eye cream, sunscreen lotion or aftersun lotion, nourishing cream,
care mask, gel pads, face lotion, moist care and cleansing wipes,
cleansing milk, cleansing soap, foam bath or shower gel, deodorant,
antiperspirant, shampoo, hair care product, hair conditioner, hair
color, hair styling agent and preferably take the form of an
emulsion, lotion, milk, fluid, cream, hydrodispersion gel, balm,
spray, alcoholic or aqueous/alcoholic solution, foam, powder,
liquid soap, tablet soap, shampoo, roll-on, stick, or makeup. In
hair treatment agents, use preferably focuses on the scalp.
[0047] It has moreover been found that a synergistically active
ternary mixture according to the invention in a concentration
sufficient to stimulate collagen synthesis has an action for
treating periodontitis and caries and in particular prevents and
delays the progress thereof. The invention accordingly teaches
advantageously making use of synergistically active ternary
mixtures according to the invention and corresponding oral care
products in any oral care or oral hygiene applications in which a
boost in collagen synthesis is associated with desired effects.
Preferably, however, the synergistically active ternary mixture or
the cosmetic, pharmaceutical or oral care preparation is used as an
active ingredient for preventing, slowing down and healing
periodontitis and caries, for treating infections of the oral
cavity and for wound healing in the oral cavity. To this end, the
ternary mixture according to the invention is preferably brought
into contact externally with the oral mucosa and the teeth. Such
mixtures and oral care formulations may in particular be used to
this end according to the invention to clean the hard tooth
structure and the oral cavity and to heal infective inflammation
and wounds in the oral cavity.
[0048] The concentration of the ternary mixtures (in liquid and/or
concentrated form) in cosmetic, oral hygiene and/or pharmaceutical
preparations (in particular for topical application) is preferably
in the range from 0.001 to 20 wt. %, preferably in the range from
0.01 to 10 wt. % and particularly preferably in the range from 0.1
to 5 wt. %, relative to the entire preparation. The mixtures
according to the invention may straightforwardly be incorporated
into conventional cosmetic or dermatological formulations such as
pump sprays, aerosol sprays, creams, ointments, tinctures, lotions,
nail care products and the like. It is here also possible and in
many cases advantageous to combine a blackberry leaf extract used
according to the invention with further active ingredients, for
example with other active ingredients against skin ageing and
wrinkles. These cosmetic and/or dermatological formulations
containing blackberry leaf extract may here otherwise be of
conventional composition and serve for treatment of the skin and/or
the hair in the manner of dermatological treatment or treatment in
the manner of cosmetic care preparations. They may, however, also
be used in makeup products in decorative cosmetics.
[0049] Preparations according to the invention containing the
ternary mixtures according to the invention may also contain
further collagen synthesis boosting active ingredients and active
ingredient combinations in particular against skin ageing and
wrinkles or for oral care (in particular against periodontitis and
caries, against inflammation of the oral mucosa and for wound
healing. According to the invention, any active ingredients
suitable or conventional for oral hygiene, for cosmetic and/or
dermatological applications may be used. Particularly preferred
ingredients are peptide substances and the derivatives thereof such
as e.g. carnitine, carnosine, creatine, matrikine peptides (e.g.
lysyl-threonyl-threonyl-lysyl-serine) and further peptide
structures such as palmitoylated pentapeptides (e.g. Matrixyl from
Sederma) or the oligopeptide with the trade name Vincipeptide (from
Vincience/France), substances such as asiatic acid, madecassic
acid, madecassoside, asiaticoside, extracts of Centella species,
niacinamide, astaxanthine, glucans e.g. from yeasts and oats, soy
extract and soy isoflavones, such as genistein and daidzein,
furthermore rutin, chrysin, morin, betel nut alkaloids, forskolin,
betulinic acid, extracts of Plantago species, extracts of Ginkgo
biloba, catechin (catechin (e.g. epigallocatechin gallate)-rich
extracts of green or black tea), polyphenois (oligomeric
procyanidins) from wine, retinoic acid, retinal, retinol, retinol
palmitate, and further retinol derivatives, glutamine, glycolic
acid and TGF-beta.
[0050] In oral hygiene applications, the ternary mixtures according
to the invention may be incorporated into the most varied dosage
forms without being limited to one or a few specific dosage forms,
as they advantageously combine harmoniously with a large number of
conventional auxiliary substances and additives. It is here
advantageous to buffer the oral hygiene products according to the
invention. A pH range from 3.5 to 10.0 is particularly advantageous
and preferred. Preferred oral hygiene products are preferably tooth
creams, toothpastes, tooth gels, mouthwashes, mouth rinses, liquids
for gargling and mouth or throat sprays and suckable pastilles,
suckable tablets, candies, chewing gums, chewable candies and
chewing gums for dental care.
[0051] It is also possible and usually advantageous for oral
hygiene purposes to combine a ternary mixture according to the
invention with other materials, in particular with MMP inhibitors,
but also for example with antimicrobially active or
antiinflammatory substances, aroma substances, flavorings and/or
auxiliary substances.
[0052] MMP inhibitors which may preferably be used in combination
are retinyl palmitate, propyl gallate, precocene,
6-hydroxy-7-methoxy-2,2-dimethyl-1(2H)-benzopyran,
3,4-dihydro-6-hydroxy-7-methoxy-2,2-dimethyl-1 (2H)-benzopyran,
benzamidine hydrochloride, the cysteine proteinase inhibitors
N-ethylmaleimide and epsilon-amino-n-caproic acid, the serine
protease inhibitor: phenylmethylsulfonyl fluoride, Collhibin (from
Pentapharm; INCI: hydrolyzed rice protein) Oenotherol (from
Soliance; INCI; propylene glycol, aqua, Oenothera biennis root
extract, ellagic acid, and ellagitannins, (e.g. from pomegranate),
phosphoramidon hinokitiol, EDTA, galardin, EquiStat (from
Collaborative Group; apple fruit extract, soy seed extract: ursolic
acid, soy isoflavones & soy proteins), sage extracts, MDI (from
Atrium; INCI: glycosaminoglycans), Fermiskin (from Silab/Mawi;
INCI: water and Lentinus edodes extract), Actimp 1.9.3. (from
Expanscience/Rahn; INCI: hydrolyzed lupine protein), Lipobelle soy
glycone (from Mibelle; INCI: alcohol, polysorbate 80, lecithin and
soy isoflavones), extracts of green and black tea and numerous
further plant extracts which are listed in WO 02/069992 (see tables
1-12).
[0053] The oral hygiene products according to the invention may
furthermore contain auxiliary materials as are conventionally used
in such preparations, e.g. preservatives, abrasives, antibacterial
agents, antiinflammatory agents, irritation-preventing agents,
irritation-suppressing agents, antimicrobial agents, antioxidants,
astringents, antiseptic agents, antistatic agents, binders,
buffers, excipients, chelating agents, cell stimulants, cleaning
agents, care agents, surface-active substances, deodorizing agents,
plasticizers, bactericides, emulsifiers, enzymes, essential oils,
film formers, fixatives, foaming agents, foam stabilizers,
substances for preventing foaming, foam boosters, gelling agent,
gel-forming agents, moisture-donating agents, moisturizing
substances, moisture-retaining substances, bleaching agents,
optical brighteners, soil-repelling agents, friction-reducing
agents, slip agents, opacifiers, hiding agents, lustrants,
polymers, powders, proteins, abrasive agents, silicones,
skin-soothing agents, skin-cleaning agents, skin-conditioning
agents, skin-healing agents, cooling agents, skin-cooling agents,
warming agents, skin-warming agents, stabilizers, suspending
agents, thickeners, vitamins, oils, waxes, fats, phospholipids,
saturated fatty acids, mono- or polyunsaturated fatty acids,
.alpha.-hydroxy acids, polyhydroxyfatty acids, liquefying agents,
dyes, color-protective agents, pigments, aromas, flavorings,
odoriferous substances or other conventional constituents of an
oral hygiene formulation such as alcohols, polyols, electrolytes,
organic solvents, sweeteners, sugar substitutes, silicas, calcium
carbonate, calcium hydrogenphosphate, aluminum oxide, fluorides,
zinc, tin, potassium, sodium and strontium salts, pyrophosphates,
hydrogen peroxide, hydroxyapatites.
[0054] If the oral hygiene product is a solution or lotion, the
solvents stated in WO2005/123101 may, for example, be used.
Mixtures of the above-stated solvents may, of course, also be
used.
[0055] Examples of flavorings or aromas which, in addition to a
ternary mixture according to the invention, may be a constituent of
an oral hygiene product according to the invention are listed e.g.
in K. Bauer, D. Garbe, H. Surburg, Common Fragrance and Flavor
Materials, 4th. Ed., Wiley-VCH, Weinheim 2001 or also in S.
Arctander, Perfume and Flavor Chemicals, Vol. I and II, Montclair,
N.J., 1969, private publication.
[0056] Examples of natural aromas which, in addition to a ternary
mixture according to the invention, may be a constituent of an oral
hygiene product according to the invention are stated in
WO2005/123101.
[0057] Examples of uniform aromas which, in addition to a ternary
mixture according to the invention, may be a constituent of an oral
hygiene product according to the invention are likewise stated in
WO2005/123101.
[0058] Compounds with a physiological cooling effect (cooling
substances) which, in addition to a ternary mixture according to
the invention, may be a constituent of an oral hygiene product
according to the invention and/or of a cosmetic, dermatological
and/or pharmaceutical product according to the invention, are
stated in WO2005/123101. Oral hygiene products which are preferred
according to the invention are those which, in addition to
l-menthol, contain at least one, particularly preferably at least
two further cooling substances.
[0059] Components which cause a warming, spicy, tingling or
prickling sensation on the skin or mucous membranes, in particular
aroma substances with a warming effect and/or pungent tasting
compounds (pungent substances) and which, in addition to a ternary
mixture according to the invention, may be a constituent of an oral
hygiene product and/or cosmetic, dermatological or pharmaceutical
product according to the invention are likewise stated in
WO2005/123101.
[0060] Further components which, in addition to a ternary mixture
according to the invention, may be a constituent of an oral hygiene
product according to the invention are e.g. substances for
improving oral hygiene, such as for example dental care and/or
refreshing substances. Substances for improving oral hygiene
include, for example, substances for combating or preventing
plaque, calculus or caries and those for combating or preventing
bad breath. Reference is made in this connection to U.S. Pat. No.
5,043,154. Examples of substances which are to be used are
furthermore stated in WO2005/123101.
[0061] An oral hygiene product according to the invention may, in
addition to a ternary mixture according to the invention, also
contain one or more antimicrobial active ingredients for improving
oral hygiene. These active ingredients may be of a hydrophilic,
amphoteric or hydrophobic nature. Examples of such active
ingredients are likewise stated in WO2005/123101.
[0062] A cosmetic, dermatological or pharmaceutical. product and/or
oral hygiene product according to the invention may, in addition to
a ternary mixture according to the invention, also contain dyes,
colorants or pigments which are likewise stated in
WO2005/123101.
[0063] Preparations serving for cosmetic, for oral hygiene and/or
for pharmaceutical purposes which contain a ternary mixture
according to the invention may particularly advantageously contain
antioxidants, it being possible to use any antioxidants which are
suitable for or usual in oral hygiene, cosmetic and/or
dermatological applications. The antioxidants selected are
advantageously those stated in WO2005/123101.
[0064] Preferred preparations serving for oral hygiene, cosmetic
and/or pharmaceutical purposes which contain a ternary mixture
according to the invention also contain one or more vitamins and/or
vitamin precursors, it being possible to use any vitamins and
vitamin precursors which are suitable for or usual in cosmetic
and/or dermatological applications. These include in particular the
vitamins and vitamin precursors already stated in
WO2005/123101.
[0065] For use in the manner conventional for cosmetics and skin
preparations, the ternary mixtures according to the invention are
applied in an adequate amount onto the skin and/or the hair.
Cosmetic and dermatological preparations which contain a ternary
mixture according to the invention and additionally act as a
sunscreen preparation offer particular advantages. These
preparations advantageously contain at least one UVA filter and/or
at least one UVB filter and/or at least one inorganic pigment. The
preparations may here assume various forms, as they are e.g.
conventionally used for sunscreen preparations. They may
accordingly form e.g. a solution, an emulsion of the water-in-oil
(W/O) or oil-in-water (O/W) type, or a multiple emulsion, for
example of the water-in-oil-in-water (W/O/W) type, a gel, a
hydrodispersion, a solid stick or also an aerosol.
[0066] Preparations according to the invention in the field of
cosmetics and skin preparations which contain a ternary mixture
according to the invention are particularly advantageously combined
with substances which absorb or reflect UV radiation, specifically
for cosmetic or skin-protecting purposes (thus not for oral hygiene
purposes), the total amount of the filter substances amounting to
from 0.01 wt. % to 40 wt. %, preferably 0.1% to 10 wt. %, in
particular 1.0 to 5.0 wt. %, relative to the total weight of the
preparations, in order to provide cosmetic preparations which
protect the hair or skin from ultraviolet radiation. These
preparations advantageously contain at least one UVA filter and/or
at least one UVB filter and/or at least one inorganic pigment, such
that a sun protection factor of at least >2 (preferably >5)
is achieved. These preparations according to the invention may here
assume various forms, as are e.g. conventionally used for sunscreen
preparations. They may accordingly be e.g. a solution, an emulsion
of the water-in-oil (W/O) or oil-in-water (O/N) type, or a multiple
emulsion, for example of the water-in-oil-in-water (W/O/W) type, a
gel, a hydrodispersion, a solid stick or also an aerosol.
[0067] Advantageous UV filters and inorganic photoprotective
pigments are stated in WO2005/123101. UV absorbers which are
particularly suitable for combining are likewise stated in
WO2005/123101.
[0068] Advantageous inorganic photoprotective pigments are finely
dispersed metal oxides and metal salts which are likewise stated in
WO2005/123101. The total amount of inorganic pigments, in
particular hydrophobic inorganic micropigments in the finished
cosmetic or dermatological formulations is advantageously in the
range from 0.1 to 30 wt. %, preferably 0.1 to 10.0, in particular
0.5 to 6.0 wt. %, relative to the total weight of the
formulations.
[0069] In many preparations, a combination with (metal) chelating
agents may also be advantageous. (Metal) chelating agents which are
preferably to be used are those compounds stated in
WO2005/123101.
[0070] Cosmetic, pharmaceutical and/or oral hygiene preparations
which are preferred according to the invention may also contain
antiinflammatory active ingredients and/or active ingredients which
relieve erythema and/or itching. Any antiinflammatory active
ingredients and any active ingredients which relieve erythema
and/or itching which are suitable for cosmetic and/or
dermatological and/or oral hygiene applications may here be used.
The compounds stated in WO2005/123101 are advantageously used as
antiinflammatory active ingredients or active ingredients which
relieve erythema and/or itching.
[0071] The amount of antirritants (one or more compounds) in the
preparations according to the invention preferably amounts to
0.0001 to 20 wt. %, particularly preferably 0.0001-10 wt. %, in
particular 0.001-5 wt. %, relative to the total weight of the
preparation.
[0072] Ternary mixtures according to the invention may likewise
advantageously be used for cosmetic and/or dermatological purposes
in combination with skin-lightening active ingredients. Any
skin-lightening active ingredients suitable for or usual in
cosmetic and/or dermatological applications which are stated in
WO2005/123101 may here be used according to the invention.
[0073] Ternary mixtures according to the invention may in
particular advantageously be used in cosmetic and dermatological
preparations in combination with insect repellents, such as e.g.
DEET, IR 3225, Dragorepel (Symrise GmbH & Co. KG).
[0074] Ternary mixtures according to the invention may furthermore
advantageously be used, in particular in cosmetic and
dermatological preparations, in combination with hair growth
inhibitors as stated in WO2005/123101.
[0075] In numerous cases, ternary mixtures according to the
invention may also advantageously be used in combination with the
osmolytes stated in WO2005/123101.
[0076] Ternary mixtures according to the invention may
advantageously be used, in particular in cosmetic and
dermatological preparations, in combination with hair care products
and antidandruff active ingredients (e.g. climbazole, ketoconazole,
piroctone olamine, zinc pyrithione).
[0077] Ternary mixtures according to the invention may also in
numerous cases advantageously be used in preparations according to
the invention in combination with one or more preservatives. The
preservatives selected are here preferably those stated in
WO2005/123101.
[0078] It is additionally preferred according to the invention to
use ternary mixtures according to the invention in combination with
substances which are primarily used for inhibiting the growth of
undesired microorganisms on or in animal organisms. Apart from
conventional preservatives, further active ingredients which may be
mentioned in addition to the large group of conventional
antibiotics are in particular the compounds stated in
WO2005/123101.
[0079] Ternary mixtures according to the invention may furthermore
also particularly advantageously be used according to the invention
in combination with antiperspirant active ingredients
(antiperspirants) for combating body odor in cosmetic,
dermatological and/or pharmaceutical preparations. Antiperspirant
active ingredients which may primarily be considered are the
compounds stated in WO2005/123101.
[0080] Ternary mixtures according to the invention may
advantageously be combined in cosmetic and dermatological
preparations with cosmetic auxiliary substances as are
conventionally used in such preparations, thus e.g. with: perfume
oils; agents for preventing foaming; dyes; pigments having a
coloring effect; thickeners; surface-active substances;
emulsifiers; softening substances; moistening and/or
moisture-retaining substances; fats; oils; waxes; other
conventional constituents of a cosmetic formulation such as
alcohols, polyols, polymers, foam stabilizers, electrolytes,
organic solvents or silicone derivatives.
[0081] A large proportion of care substances is often advantageous
in formulations for topical prophylactic or cosmetic treatment of
the skin which contain ternary mixtures according to the invention.
According to a preferred embodiment, the compositions contain one
or more of the stated animal- and/or plant-based care products
stated in WO2005/123101.
[0082] The animal and/or plant protein hydrolysates stated in
WO2005/123101 may advantageously also be added to the ternary
mixture according to the invention.
[0083] Where a cosmetic or dermatological preparation containing a
ternary mixture according to the invention is a solution or lotion,
the solvents stated in WO2005/123101 may advantageously be
used.
[0084] Cosmetic preparations according to the invention which
contain a ternary mixture according to the invention may
advantageously also contain the moisture-retaining regulators
stated in WO2005/123101.
[0085] In preferred embodiments of the invention, cosmetic
preparations which contain a ternary mixture according to the
invention may also contain mono-, di- and oligosaccharides.
[0086] It is furthermore preferred for cosmetic preparations which
contain a ternary mixture according to the invention to contain one
or more further plant extracts which are conventionally produced by
extracting the entire plant, but in individual cases also just
flowers and/or leaves, wood, bark or roots of the plant. With
regard to the plant extracts usable for cosmetic, pharmaceutical
and/or dermatological purposes, a person skilled in the art will
refer to the table beginning on page 44 of the 3rd edition of the
"Leitfaden zur Inhaltsstoffdeklaration kosmetischer Mittel"
["Guidelines for the nomenclature of ingredients in cosmetic
agents"], published by the German Cosmetic, Toiletry, Perfumery and
Detergent Association (IKW), Frankfurt. The extracts stated in
WO2005/123101 are advantageously suitable for cosmetic,
dermatological, pharmaceutical and/or oral hygiene purposes.
[0087] According to the invention, cosmetic preparations which
contain a ternary mixture according to the invention may, in
particular if crystalline or microcrystalline solids, for example
inorganic micropigments, are to be incorporated into the
preparations, may also contain the anionic, cationic, nonionic
and/or amphoteric surfactants stated in WO2005/123101.
[0088] The surface-active substance may be present in the
preparations according to the invention in a concentration of
between 1 and 98 wt. %, relative to the total weight of the
preparations.
[0089] Cosmetic or dermatological preparations which contain a
ternary mixture according to the invention may also assume emulsion
form.
[0090] The oil phase of cosmetic, dermatological and/or
pharmaceutical preparations according to the invention may
advantageously be selected from groups of substances stated in
WO2005/123101.
[0091] Preparations according to the invention which assume
emulsion form advantageously comprise one or more emulsifiers. O/W
emulsifiers may, for example, advantageously be selected from the
group of products stated in WO2005/123101.
[0092] Preferred developments and further aspects of the present
invention are revealed by the attached claims and the following
Examples together with the tables, the examples not being intended
to limit the invention:
EXAMPLE 1
[0093] Method for determining the collagen synthesis boosting
activity of selected substances of natural or synthetic origin.
[0094] Fibroblasts are responsible for collagen synthesis in the
dermis layer of the skin. The test system involves culturing normal
human dermal fibroblasts (NHDF) in a "monolayer" culture in 96 well
MTPs, incubating them over a defined period with test substances
and then determining the increase in collagen qualitatively by a
staining method.
[0095] The principle of the assay is based on histological,
specific staining of the soluble collagen (predominantly type I and
III collagen) with the assistance of the dye Sirius Red (Direct Red
80). Sirius Red is an anionic dye having sulfonic acid groups
attached to its side chains. These sulfonic acid groups react with
the side chain groups of the amino acids (proline, hydroxyproline,
lysine and hydroxylysine) predominantly occurring in collagen, it
being necessary for an intact collagen structure to be present.
##STR00001##
[0096] The model used for the assay design is the procedure
described in B. J. Walsh et al., Analytical Biochemistry 203,
187-190 (1992) for the quantitative determination of collagen on
the 96 well scale.
[0097] The test substance's collagen synthesis boosting effect is
tested on in vitro aged (>8th passage) NHDF in 96 well
microtiter plates (2*10.sup.4 cells per well). A suitable solvent
must first be identified for each test sample by preparing a stock
solution of the test sample. The incubation solutions of the test
substance are then produced in DMEM supplemented with 0.2% BSA.
Possible solvents should be present in an amount of at most 0.2% in
all dilutions of the incubation solution. The maximum usage
concentration of the test substance is based on the IC.sub.20
values obtained in the cytotoxicity investigation (resazurin assay
on 3T3 mouse fibroblasts) and is set at 0.1*IC.sub.20.
[0098] After a 24 h adaptation phase for the NHDF, the cells are
incubated (37.degree. C., 5% CO.sub.2) for 48 h with the incubation
solution and corresponding control solutions (solvent and blank).
In order to be able to identify possible influences of the test
substances on the subsequent staining procedure, the highest usage
concentration of the test substances is also simultaneously
processed without cells as a background control. The cells are then
disrupted by a double freeze/thaw cycle (-20.degree. C./-80.degree.
C./37.degree. C./-80.degree. C./37.degree. C.; 10 minutes each) and
96 hours' evaporation (24 h moist heat at 37.degree. C., 72 h dry
heat at 30.degree. C.). The resultant collagen-coated wells can be
stained the Sirius Red dye (0.1% solution). The dye bound to the
collagen is brought back into solution by a triple washing step
with 0.01 mM HCl solution and subsequent incubation (at least 5
minutes) with 0.1 mM NaOH solution. The absorption of the resultant
dye solution can be determined photometrically at 540 nm.
[0099] Thanks to the linear relationship between collagen content
and the OD values arising from staining, the increase in OD is
determined for qualitative assessment of the collagen synthesis
boosting effect. To this end, the mean and standard deviations of
the controls and the test samples are calculated and then a
background or blank correction is made. The increase in OD is then
obtained from the relationship between the cells which have been
treated (with test substance) and those which have not been treated
(only with solvent or medium).
Sources:
[0100] 1. Walsh B. J., Thornton S. C., Penny R. and Breit S. N.:
Microplate Reader-Based Quantitation of Collagens; Analytical
Biochemistry 203, 187-190 (1992) [0101] 2. Nethery A., Lyons J. G.
and O'Grady R. L.: A Spectrometric Collagenase Assay: Analytical
Biochemistry 159, 390-395 (1986)
EXAMPLE 2
[0102] Determination of the synergistically enhanced collagen
synthesis boosting activity of selected ternary mixtures containing
at least one extract of an Aloe species, at least one substance
from the group ascorbic acid and the derivatives thereof and at
least one rosaceous plant extract, preferably raspberry leaf
extract, strawberry leaf extract, blackberry leaf extract or
meadowsweet herb extract.
[0103] The potentially synergistically enhanced activities of
ternary mixtures containing Aloe extract, at least one substance
from the group ascorbic acid and the derivatives thereof and at
least one rosaceous plant extract, preferably raspberry leaf
extract, strawberry leaf extract, blackberry leaf extract or
meadowsweet herb extract were determined by ascertaining the
collagen synthesis boosting characteristics both for the individual
substances and for different ternary mixtures in accordance with
the test method described in Example 1. The results of the
investigations are listed in Table 1.
TABLE-US-00001 TABLE 1 Collagen synthesis boost of magnesium
ascorbyl phosphate, Aloe extract, raspberry leaf extract,
strawberry leaf extract, meadowsweet herb extract and ternary
mixtures containing (i) magnesium ascorbyl phosphate, Aloe extract
and meadowsweet herb extract, (ii) magnesium ascorbyl phosphate,
Aloe extract and strawberry leaf extract, (iii) magnesium ascorbyl
phosphate, Aloe extract and raspberry leaf extract and (iiii)
magnesium ascorbyl phosphate, Aloe extract and blackberry leaf
extract; boost in % relative to untreated control Collagen
synthesis boost Usage concentration [%], relative to Synergy
[mg/ml] untreated control index SI Aloe extract (Bio505) 10.860
45.70 --/-- Magnesium ascorbyl 0.362 66.97 --/-- phosphate (Bio172)
Meadowsweet herb 0.030 14.22 --/-- extract (Bio1544) Ternary
mixture 3.620 (Bio505) + 112.76 3.99 (Bio505 + Bio172 + 0.121
(Bio172) + Bio1544) 0.010 (Bio1544) Aloe extract (Bio505) 10.860
45.70 --/-- Magnesium ascorbyl 0.362 66.97 --/-- phosphate (Bio172)
Strawberry leaf 0.030 14.85 --/-- extract (Bio1545) Ternary mixture
3.620 (Bio505) + 96.37 3.31 (Bio505 + Bio172 + 0.121 (Bio172) +
Bio1545) 0.010 (Bio1545) Aloe extract (Bio505) 10.860 47.59 --/--
Magnesium ascorbyl 0.362 67.44 --/-- phosphate (Bio172) Raspberry
leaf 0.030 16.74 --/-- extract (Bio 615) Ternary mixture 3.620
(Bio505) + 142.15 4.48 (Bio505 + Bio172 + 0.121 (Bio172) + Bio615)
0.010 (Bio615) Magnesium ascorbyl 0.362 66.97 --/-- phosphate
(Bio172) Aloe extract (Bio505) 10.860 45.70 --/-- Blackberry leaf
0.003 14.15 --/-- extract (Bio684/4) Ternary mixture 3.620 (Bio505)
+ 153.93 5.46 (Bio505 + Bio172 + 0.121 (Bio172) + Bio684/4) 0.010
(Bio684/4)
Result:
[0104] The synergy index (SI) values of the ternary mixtures
according to the invention were calculated according to Kull
(literature: F. C. Kull et al, Applied Microbiology vol. 9, p.
538-541 (1961); D. C. Steinberg, Cosmetics & Toiletries vol.
115(11), 59-62 (2000) by means of the following equation.
SI=Z*D/A+Z*E/B+Z*F/C
where: D, E, F: proportion factor for the individual constituents
(e.g., 33 weight percent=factor 0.33) A, B, C: collagen stimulation
of the individual substances (increase in %, relative to control
without active ingredient) Z: collagen stimulation of the ternary
mixture (increase in %, relative to control without active
ingredient)
[0105] A synergistic effect is present if values of greater than
1.00 are obtained. Values of less than 1.00 indicate an
antagonistic effect. A value of exactly 1.00 indicates an effect
which is neither synergistic nor antagonistic.
[0106] An example calculation is show below for the ternary mixture
containing in each case one third (D, E and F factor in each case
0.33) of the amounts of magnesium ascorbyl phosphate, Aloe extract
and raspberry leaf extract used in the individual experiment.
SI=142.15*033/67.44+142.15*0.33/47.59+142.15*0.33/16.74=4.48
[0107] The SI value of 4.48 shows a significant, synergistically
enhanced effect of the mixture containing magnesium ascorbyl
phosphate, Aloe extract and raspberry leaf extract. The SI values
of the further investigated ternary mixtures are shown in Table
1.
[0108] The results shown in Table 1 and, in particular, the
calculated synergy index values unambiguously show that the ternary
mixtures according to the invention containing: Aloe extract,
magnesium ascorbyl phosphate, and a rosaceous plant extract
(according to Table 1 e.g. raspberry leaf extract, strawberry leaf
extract, blackberry leaf extract or meadowsweet herb extract) at a
quantity ratio of 96.51 weight percent Aloe to 3.22 weight percent
magnesium ascorbyl phosphate, to 0.27% weight percent rosaceous
plant extracts, exhibit a synergistically enhanced collagen
synthesis boosting activity. In the case of the ternary mixture
containing Aloe extract, magnesium ascorbyl phosphate and
strawberry leaf extract, it proved possible to boost collagen
synthesis by 96.37% when using in each case one third of the total
amount (synergy index: 3.31). In the case of the ternary mixture
containing Aloe extract, magnesium ascorbyl phosphate and
meadowsweet herb extract, it proved possible to boost collagen
synthesis by 112.76% when using in each case one third of the total
amount (synergy index: 3.99). It proved possible to achieve the
greatest boost in collagen synthesis by 142.15% or 153.93% when
using in each case one third of the total amount for the ternary
mixture containing Aloe extract, magnesium ascorbyl phosphate and
raspberry leaf extract or blackberry leaf extract respectively
(synergy index values: 4.48 and 5.46). Since synergy index values
of greater than 1 were determined in every case, the synergistic
effect of the ternary mixtures according to the invention has been
unambiguously proven.
EXAMPLE 3
[0109] Determination of the synergistically enhanced collagen
synthesis boosting activity of further ternary mixtures containing
(i) Aloe extract, (ii) magnesium ascorbyl phosphate or sodium
ascorbyl phosphate and (iii) raspberry leaf extract:
[0110] Example 3 shows further ternary mixtures having mixture
ratios modified relative to Example 2, in which it likewise proved
possible to identify a synergistically enhanced activity of the
ternary mixtures. The results of the investigations are listed in
Table 2.
TABLE-US-00002 TABLE 2 Collagen synthesis boost of Aloe extract,
magnesium ascorbyl phosphate, sodium ascorbyl phosphate, raspberry
leaf extract and ternary mixture containing (i) Aloe extract, (ii)
magnesium ascorbyl phosphate or sodium ascorbyl phosphate and (iii)
raspberry leaf extract; boost in % relative to untreated control.
Collagen synthesis boost Usage concentration [%], relative to
Synergy [mg/ml] untreated control index SI Aloe extract (Bio505)
10.110 39.87 --/-- Magnesium ascorbyl 1.020 141.13 --/-- phosphate
(Bio1300/1) Sodium ascorbyl 1.020 144.57 --/-- phosphate (Bio1586)
Raspberry leaf 0.12 9.93 --/-- extract (Bio 615) Ternary mixture A
3.370 (Bio505) + 160.52 7.04 (Bio505 + 0.340 (Bio . . . ) +
Bio1300/1 + Bio615) 0.040 (Bio615) Ternary mixture B 3.370 (Bio505)
+ 94.95 4.16 (Bio505 + Bio1586 + 0.340 (Bio . . . ) + Bio615)
0.040(Bio615)
Result:
[0111] The results listed in Table 2 show that further ternary
mixtures according to the invention containing: Aloe extract,
magnesium ascorbyl phosphate, and raspberry leaf extract or Aloe
extract, sodium ascorbyl phosphate and raspberry leaf extract in a
quantity ratio of 90 weight percent Aloe extract to 9 weight
percent magnesium ascorbyl phosphate (or 9 weight percent sodium
ascorbyl phosphate) to 1 weight percent raspberry leaf extract
likewise exhibit a synergistically enhanced, collagen synthesis
boosting activity. In the case of the ternary mixture containing
Aloe extract, magnesium ascorbyl phosphate and raspberry leaf
extract, it proved possible to boost collagen synthesis by 160.52%
(synergy index: 7.04) when using in each case one third of the
tested amount of individual substances. In the case of the ternary
mixture containing (ii) Aloe extract, sodium ascorbyl phosphate and
raspberry leaf extract, it proved possible to boost collagen
synthesis by 94.95% (synergy index 4.16) when using in each case
one third of the tested amount of individual substances. Since
synergy index values of greater than 1 were determined in both
cases, the synergistic effect of the ternary mixtures according to
the invention has been unambiguously proven.
EXAMPLE 4
Further Cosmetic/Dermatological Examples of Application
[0112] The dermatological and cosmetic preparations containing
synergistically active ternary mixtures in combination with other
cosmetic active ingredients and additives were used by being
applied in a sufficient amount onto the skin and/or the hair in the
manner conventional for cosmetics. Advantageous preparations for
some applications are stated by way of example below.
4.1 Antiwrinkle W/O Cream
TABLE-US-00003 [0113] Raw material name Content Part (manufacturer)
INCI name in wt. % A Dragosan W/O P Sorbitan isostearate, 8.00
(Symrise) hydrogenated castor oil, ceresin, beeswax (cera alba)
Dragoxat EH (Symrise) Ethylhexyl 8.00 ethylhexanoate Isodragol
(Symrise) Triisononanoin 8.00 Dow Corning 200 Fluid Dimethicone
2.00 (300 cs) (Dow Corning) Betone Gel Mio Mineral oil, 3.00
(Elementis) quaternium-18 hectorite, propylene carbonate B
Demineralized water Water (aqua) ad 100 Magnesium sulfate Magnesium
sulfate 1.00 heptahydrate (Merck) Glycerin, 99.5% Glycerin 3.00
Drago-Beta-Glucan Water (aqua), butylene 5.00 (Symrise) glycol,
glycerin, Avena sativa (oat) kernel extract Raspberry leaf extract
0.005 Aloe extract 0.450 Magnesium ascorbyl 0.045 phosphate
Dragocid Liquid (Symrise) Phenoxyethanol, 0.80 methylparaben,
ethylparaben, butylparaben, propylparaben, isobutylparaben C
Symrise perfume oil Fragrance 0.30
[0114] Heat parts A and B to 75.degree. C. without
Drago-Beta-Glucan, Add Drago-Beta-Glucan to part B. Add part B to
part A and emulsify. Stir emulsion until cold, homogenize once more
at approx, 50.degree. C. and add perfume oil at approx. 35.degree.
C.
4.2 Night Cream Against Skin Ageing
TABLE-US-00004 [0115] Raw material name Content in wt. Part
(manufacturer) INCI name % A Dragosan W/O P (Symrise) Sorbitan
isostearate, 6.00 hydrogenated castor oil, ceresin, beeswax (cera
alba) PCL Liquid (Symrise) Cetearyl ethylhexanoate, 12.00 isopropyl
myristate Sunflower oil (H. Erhard Helianthus annuus (sunflower)
5.00 Wagner) seed oil Sweet almond oil (H. Erhard Prunus dulcis
5.00 Wagner) Dragosan W/O Liquid Polyglyceryl-3 polyricinoleate,
1.00 (Symrise) sorbitan isostearate Alugel 34 TH (Baerlocher)
Aluminium stearate 1.00 Oxynex 2004 (Merck) BHT 0.10 B
Demineralized water Water (aqua) ad 100 Glycerin, 99.5% Glycerin
2.00 Karion F (Merck) Sorbitol 2.00 Aloe Vera Gel Concentrate Water
(aqua), Aloe barbadensis 3.00 10/1 (Symrise) leaf juice Extrapon
witch hazel Propylene glycol, Hamamelis 1.00 distillate colorless
(Symrise) virginiana (witch hazel) water, water (aqua), Hamamelis
virginiana (witch hazel) extract Strawberry leaf extract 0.040 Aloe
extract 2.000 Sodium ascorbyl 0.400 phosphate Magnesium sulfate
Magnesium sulfate 0.70 heptahydrate (Merck) Dragocid Liquid
(Symrise) Phenoxyethanol, 0.80 methylparaben, ethylparaben,
butylparaben, propylparaben, isobutylparaben C Vitamin E acetate
(DSM Tocopheryl acetate 3.00 Nutritional Products) Vitamin A
palmitate in oil (1 Retinyl palmitate 0.20 million IU/g) (DSM
Nutritional Products) -(-alpha-)-Bisabolol, natural Bisabolol 0.10
(Symrise) Symrise perfume oil Fragrance 0.40
[0116] Heat parts A and B separately to approx. 80.degree. C. Add
part B to part A, emulsify and stir until cold. At approx.
60.degree. C., homogenize once more and add part C at approx.
35.degree. C.
4.3 O/W Lotion Against Skin Ageing with UVA/B Broadband
Protection
TABLE-US-00005 Raw material name Content in wt. Part (manufacturer)
INCI name % A Emulsiphos (Symrise) Potassium cetyl phosphate, 1.50
hydrogenated palm glycerides Tegosoft TN (Degussa) C12-15 alkyl
benzoate 5.00 Copherol 1250 (Cognis) Tocopheryl acetate 0.50
Lanette O (Cognis) Cetearyl alcohol 1.00 Neutral oil (Symrise)
Caprylic/capric triglyceride 2.00 Dow Corning 246 Fluid (Dow
Cyclohexasiloxane (and) 2.00 Corning) cyclopentasiloxane Neo
Heliopan AV (Symrise) Ethylhexyl methoxycinnamate 3.00 Neo Heliopan
OS (Symrise) Ethylhexyl salicylate 5.00 Neo Heliopan MBC
4-Methylbenzylidene camphor 1.50 (Symrise) Neo Heliopan 357
(Symrise) Butyl methoxydibenzoylmethane 1.00 EDETA DB (BASF)
Disodium EDTA 0.10 Keltrol T (Danby-Chemie) Xanthan gum 0.20
Carbopol ETD 2050 Carbomer 0.20 (Noveon) B Demineralized water
Water (aqua) ad 100 Glycerin, 99.5% Glycerin 4.70 Dragocid liquid
(Symrise) Phenoxyethanol, 0.70 methylparaben, ethylparaben,
butylparaben, propylparaben, isobutylparaben Neo Heliopan .RTM. AP
(22% aq. Disodium phenyl 4.55 solution neutralized with
dibenzimidazole tetrasulfonate triethanolamine) (Symrise) Neo
Heliopan Hydro (30% Phenylbenzimidazole sulfonic 6.67 aq. solution
neutralized with acid triethanolamine) (Symrise) Strawberry leaf
extract 0.10 Aloe extract 1.80 Magnesium ascorbyl 0.60 phosphate C
Triethanolamine, 99% Triethanolamine 0.50 D Symrise perfume oil
Fragrance 0.40 Dragosantol (Symrise) Bisabolol 0.10
[0117] Heat part A (apart from Keltrol and Carbopol) to 85.degree.
C. Add Keltrot and Carbopol and homogenize. Heat part B to
85.degree. C. and add part B to part A. Add part C directly to part
A/B, homogenize and leave to cool. Add part D to part A/B/C and
homogenize. The pH value of the final product should be approx. 7.2
to 7.5.
4.4 Aftersun Lotion (O/W) Against Skin Ageing
TABLE-US-00006 [0118] Raw material name Content in wt. Part
(manufacturer) INCI name % A Demineralized water Water (aqua) ad
100 Glycerin, 99.5% Glycerin 4.00 D-Panthenol (BASF) Panthenol 1.00
Butylene glycol Butylene glycol 5.00 Allantoin (Merck) Allantoin
0.10 Aloe Vera Gel Concentrate Water (aqua), Aloe barbadensis 3.0
10/1 (Symrise) leaf juice Raspberry leaf extract 0.10 Aloe extract
1.50 Sodium ascorbyl 0.50 phosphate Lara Care A-200 (Rahn)
Galactoarabinan 0.25 B Baysilone Oil M 350 (GE Dimethicone 1.00
Bayer Silicones) Copherol 1250 (Cognis) Tocopheryl acetate 0.50
Tegosoft TN (Degussa) C12-15 alkyl benzoate 5.00 Cetiol SB 45
(Cognis) Butyrospermum parkii (Shea 1.00 butter) Cetiol OE (Cognis)
Dicaprylyl ether 4.00 -(-alpha-)-Bisabolol, natural Bisabolol 0.10
(Symrise) Dragocid Liquid (Symrise) Phenoxyethanol, 0.70
methylparaben, ethylparaben, butylparaben, propylparaben,
isobutylparaben Pemulen TR-2 (Noveon) Acrylates/C10-30 alkyl
acrylate 0.25 crosspolymer Frescolat ML cryst. (Symrise) Menthyl
lactate 0.80 Symrise perfume oil Fragrance 0.30 C Sodium hydroxide
(10% aq. Sodium hydroxide 0.60 solution)
[0119] Dissolve part A in water. Dissolve Frescolat ML cryst. and
Cetiol SB 45 from part B with heating to at most 35.degree. C. in
Tegosoft Tenn., leave to cool and add the remaining constituents of
part B. Add part B to part A with stirring and homogenize. The pH
value of the final product should be approx. 6.0.
4.5 Bodyspray O/W Against Skin Ageing
TABLE-US-00007 [0120] Raw material name Content Part (manufacturer)
INCI name in wt. % A Dracorin GOC (Symrise) Glyceryl oleate
citrate, 2.00 caprylic/capric triglyceride Neutral oil
Caprylic/capric triglyceride 4.00 Paraffin oil 5 E Paraffinum
liquidum 4.00 (Parafluid) PCL Liquid 100 Cetearyl ethylhexanoate
7.00 (Symrise) Dragoxat EH (Symrise) Ethylhexyl ethylhexanoate 4.00
Dow Corning 345 Fluid Cyclomethicone 0.50 (Dow Corning) Dragosantol
(Symrise) Bisabolol 0.10 Symrise perfume oil Fragrance 0.20 B
Demineralized water Water (aqua) ad 100 Pemulen TR-2 (Noveon)
Acrylates/C10-30 alkyl 0.20 acrylate crosspolymer Hydrolite-5
(Symrise) Pentylene glycol 5.00 Drago-Oat-Active Water (aqua),
butylene 1.00 (Symrise) glycol, Avena sativa (oat) kernel extract
Raspberry leaf extract 0.001 Aloe extract 0.990 Sodium ascorbyl
0.020 phosphate C Sodium hydroxide Sodium hydroxide 0.40 (10% aq.
solution)
[0121] Swell Pemulen in water, then add the remaining raw materials
of part B. Mix part A. Add part B to part A without stirring and
only then emulsify. Add part C during emulsification. The pH value
of the final product should be approx. 6.3.
4.6 O/W Cream Against Skin Ageing
TABLE-US-00008 [0122] Raw material name Content Part (manufacturer)
INCI name in wt. % A Dracorin GMS (Symrise) Glyceryl stearate 2.00
PCL Solid (Symrise) Stearyl heptanoate, stearyl 2.00 caprylate
Lanette O (Cognis) Cetearyl alcohol 3.00 PCL Liquid 100 Cetearyl
ethylhexanoate 5.00 (Symrise) Isodragol (Symrise) Triisononanoin
2.00 Abil 350 (Degussa- Dimethicone 2.00 Goldschmidt) Dragoxat EH
(Symrise) Ethylhexyl ethylhexanoate 3.00 B Demineralized water
Water (aqua) ad 100 Carbopol Ultrez-10 Carbomer 0.10 (Noveon)
Keltrol RD (CP-Kelco) Xanthan gum 0.10 Emulsiphos (Symrise)
Potassium cetyl phosphate, 2.00 hydrogenated palm glycerides
Dragocid Liquid Phenoxyethanol, 0.80 (Symrise) methylparaben,
ethylparaben, butylparaben, propylparaben, isobutylparaben Extrapon
Chamomile Glycerin, water (aqua), 0.50 GW (Symrise) Chamomilla
recutita (matricaria) flower extract Extrapon Rosemary GW Glycerin,
water (aqua), 0.30 (Symrise) Rosmarinus officinalis (rosemary) leaf
extract Extrapon Green Tea GW Glycerin, water (aqua), 0.20
(Symrise) Camellia sinensis leaf extract Meadowsweet herb 0.960
extract Aloe extract 0.030 Magnesium ascorbyl 0.003 phosphate
1,2-Propylene glycol 99P Propylene glycol 5.00 GC Glycerin 85P
Glycerin 2.00 C Sodium hydroxide Sodium hydroxide 0.25 (10% aq.
solution) D Symrise perfume oil Fragrance 0.30
[0123] Preswell Carbopol Ultrez 10 and Keltrol RD in the water and
add the remaining raw materials of part B thereto. Heat parts A and
B separately to approx. 80.degree. C. Add part A to part B and
emulsify while adding part C. Stir until cold and add part D at
approx. 35.degree. C. The pH value of the final product should be
approx. 5.5.
4.7 Shampoo Against Skin Ageing
TABLE-US-00009 [0124] Raw material name Content in Part
(manufacturer) INCI name wt. % A Genapol LRO liquid (Cognis) Sodium
laureth sulfate 37.00 Dragoderm (Symrise) Glycerin, Triticum 2.00
vulgare (wheat) gluten, water (aqua) Raspberry leaf extract 0.01
Aloe extract 0.9 Magnesium ascorbyl 0.09 phosphate B Demineralized
water Water (aqua) ad 100 Merquat 550 (Ondeo Nalco)
Polyquaternium-7 0.50 C Demineralized water Water (aqua) 20.00
Comperlan 100 (Cognis) Cocamide MEA 0.50 D Tego Betaine L7
unpreserved Cocamidopropyl 6.00 (Degussa-Goldschmidt) betaine
Citric acid 10% Citric acid 0.30 EDETA B powder (BASF) Tetrasodium
EDTA 0.10 Sodium benzoate Sodium benzoate 0.50 Sodium chloride
Sodium chloride 1.00 Symrise perfume oil Fragrance 0.50
[0125] Dissolve Dragoderm and blackberry leaf extract in Genapol
LRO. Predissolve Merquat 550 in water and add. Dissolve part C with
stirring and heating and leave to cool. Dissolve part C in part
A/B. Add the raw materials of part D in succession and stir. The pH
value of the final product should be approx. 5.0.
4.8 O/W Cream Against Skin Ageing
TABLE-US-00010 [0126] Raw material name Content Part (manufacturer)
INCI name in wt. % A Dracorin CE (Symrise) Glyceryl stearate
citrate 5.00 Neutral oil (Symrise) Caprylic/capric triglyceride
6.00 Isopropyl palmitate Isopropyl palmitate 4.00 (Symrise) Lanette
16 (Cognis) Cetyl alcohol 1.00 PCL Liquid 100 Cetearyl
ethylhexanoate 3.00 (Symrise) Dragoxat EH (Symrise) Ethylhexyl
ethylhexanoate 3.00 Abil 350 (Degussa- Dimethicone 0.50
Goldschmidt) B Demineralized water Water (aqua) ad 100 Keltrol RD
(Rahn) Xanthan gum 0.20 Symdiol 68 (Symrise) 1,2-Hexanediol,
caprylyl 0.50 glycol Drago-Beta-Glucan Water (aqua), butylene 0.30
(Symrise) glycol, glycerin, Avena sativa (oat) kernel extract
Blackberry leaf extract 0.02 Aloe extract 1.80 Sodium ascorbyl 0.18
phosphate Glycerin 85P Glycerin 3.00 C Symrise perfume oil
Fragrance 0.30
[0127] Swell Keltrol in water and add the remaining raw materials
of part B to Drago-Beta-Glucan. Heat parts A and B separately to
approx. 80.degree. C. Add Drago-Beta-Glucan to part B. Add part B
to part A and only then emulsify. Stir until cold and add part C at
approx. 35.degree. C. The pH value of the final product should be
approx. 5.5.
EXAMPLE 5
Further Examples of Application in the Field of Oral Hygiene
[0128] The oral hygiene products containing synergistically active
ternary leaf extract according to the invention are applied by
being introduced in a sufficient amount into the oral cavity in the
conventional manner in combination with other active ingredients
and additives. Advantageous preparations for some applications are
stated by way of example below. Unless otherwise stated, all stated
values relate to weight.
5.1. Gel Tooth Cream with Activity Against Bad Breath
TABLE-US-00011 I (%) II (%) III (%) Na carboxymethylcellulose 0.40
0.40 0.40 Sorbitol 70%, in water 72.00 72.00 72.00 Polyethylene
glycol (PEG) 1500 3.00 3.00 3.00 Na saccharinate 0.07 0.07 0.07 Na
fluoride 0.24 0.24 0.24 p-Hydroxybenzoic acid (PHB) ethyl 0.15 0.15
0.15 ester Aroma A (see below) 0.10 0.80 0.75 Ternary mixture of
Aloe extract, 0.01 0.40 1.00 sodium ascorbyl phosphate and
raspberry leaf extract (quantity ratio: 90:9:1 w/w/w) Abrasive
silica 11.00 11.00 11.00 Thickening silica 6.00 6.00 6.00 Sodium
dodecyl sulfate (SDS) 1.40 1.40 1.40 Water, dist. ad 100.00 ad
100.00 ad 100.00
[0129] Aroma A was of the following composition:
30 wt. % I-menthol, 30 wt. % peppermint oil Mentha piperita, 21.5
wt. % peppermint oil Mentha arvensis, 9 wt. % anethole, 0.5 wt. %
anisaldehyde, 2 wt. % eucalyptol, 1 wt. % Eucalyptus globulus oil,
3 wt. % menthone, 1 wt. % spearmint oil, 1 wt. % basil oil, 0.5 wt.
% menthyl acetate, 0.05 wt. % menthyl lactate, 0.1 wt. %
menthyl-3-carboxylic acid-N-ethylamide (WS-3), 0.06 wt. %
2-hydroxyethylmenthyl carbonate (Frescolat MGC, Symrise), 0.05 wt.
% 2-hydroxypropylmenthyl carbonate, (Frescolat MPC, Symrise), 0.1
wt. % pinene, 0.1 wt. % propylene glycol, 0.05 wt. % limonene. 5.2.
Tooth Cream with Activity Against Plaque
TABLE-US-00012 I (%) II (%) III (%) Na carboxymethylcellulose 1.00
1.00 1.00 Glycerin 12.50 12.50 12.50 Sorbitol 70%, in water 29.00
29.00 29.00 Na saccharinate 0.20 0.20 0.20 Na fluoride 0.22 0.22
0.22 Azacycloheptane-2,2-diphosphoric 1.00 1.00 1.00 acid, disodium
salt Bromochlorophene 0.10 0.10 0.10 Peppermint aroma 0.05 1.10
0.35 Ternary mixture of Aloe extract, 1.05 1.30 1.70 magnesium
ascorbyl phosphate and raspberry leaf extract (quantity ratio:
90:9:1 w/w/w) Chamomile extract (Cremogen Forte 0.20 0.50 0.10
Chamomile, Symrise) Sage extract (Extrapon Sage GW, 0.20 0.10 0.30
Symrise) Abrasive silica 14.00 14.00 14.00 Thickening silica 5.00
5.00 5.00 Sodium dodecyl sulfate (SDS 1.50 1.50 1.50 Water, dist.
ad 100.00 ad 100.00 ad 100.00
5.3. Tooth Cream with Activity Against Plaque
[0130] Base: silica, alkali metal diphosphate
TABLE-US-00013 I (%) II (%) III (%) Carragenan 0.90 0.90 0.90
Glycerin 15.00 15.00 15.00 Sorbitol 70%, in water 25.00 25.00 25.00
PEG 1000 3.00 3.00 3.00 Na fluoride 0.24 0.24 0.24 Tetrapotassium
diphosphate 4.50 4.50 4.50 Tetrasodium diphosphate 1.50 1.50 1.50
Na saccharinate 0.40 0.40 0.40 Precipitated silica 20.00 20.00
20.00 Titanium dioxide 1.00 1.00 1.00 PHB methyl ester 0.10 0.10
0.10 Menthol/eucalyptol aroma 1.10 0.80 0.20 Ternary mixture of
Aloe 0.10 0.40 1.00 extract, sodium ascorbyl phosphate and
blackberry leaf extract (quantity ratio: 90:9:1 w/w/w) Sodium
dodecyl sulfate 1.30 1.30 1.30 Water, dist. ad 100.00 ad 100.00 ad
100.00
5.4. Tooth Cream for Sensitive Teeth
TABLE-US-00014 [0131] I (%) II (%) III (%) Na
carboxymethylcellulose 0.70 0.70 0.70 Xanthan Gum 0.50 0.50 0.50
Glycerin 15.00 15.00 15.00 Sorbitol 70%, in water 12.00 12.00 12.00
K nitrate 5.00 5.00 5.00 Na monofluorophosphate 0.80 0.80 0.80 PHB
methyl ester 0.15 0.15 0.15 PHB propyl ester 0.05 0.05 0.05 Na
saccharinate 0.20 0.20 0.20 Menthol/anethole aroma 0.25 0.75 0.25
Ternary mixture of Aloe 0.02 1.00 1.50 extract, sodium ascorbyl
phosphate and raspberry leaf extract (quantity ratio: 90:9:1 w/w/w)
Rosemary extract (Extrapon 0.20 0.01 0.10 Rosemary, Symrise) Ca
carbonate 35.00 35.00 35.00 Silicon dioxide 1.00 1.00 1.00 Sodium
dodecyl sulfate 1.50 1.50 1.50 (SDS) Water, dist. ad 100.00 ad
100.00 ad 100.00
5.5. Tooth Cream for Sensitive Teeth
TABLE-US-00015 [0132] I (%) II (%) III (%) Hydroxyethylcellulose
1.40 1.40 1.40 Guar gum 0.60 0.60 0.60 Glycerin 18.00 18.00 18.00
Sorbitol 70%, in water 12.00 12.00 12.00 Na saccharinate 0.35 0.35
0.35 Dye 0.01 0.01 0.01 PHB methyl ester 0.15 0.15 0.15 PHB propyl
ester 0.04 0.04 0.04 Sr chloride 10.50 10.50 10.50
Peppermint/aniseed 0.35 1.20 0.60 aroma Ternary mixture of Aloe
0.05 0.50 0.90 extract, magnesium ascorbyl phosphate and blackberry
leaf extract (quantity ratio: 90:9:1 w/w/w) Green tea extract 0.25
0.10 0.05 (Extrapon Green Tea GW, Symrise) Precipitated silica
15.00 15.00 15.00 Silicon dioxide 1.60 1.60 1.60 Sodium dodecyl
sulfate 1.30 1.30 1.30 Water, dist. ad 100.00 ad 100.00 ad
100.00
5.6. Ready-to-Use Mouthwash with Fluoride
TABLE-US-00016 I (%) II (%) III (%) Ethanol 7.00 7.00 7.00 Glycerin
12.00 12.00 12.00 Na fluoride 0.05 0.05 0.05 Pluronic F-127 .RTM.
(BASF, 1.40 1.40 1.40 surface-active substance) Na phosphate buffer
pH 7.0 1.10 1.10 1.10 Sorbic acid 0.20 0.20 0.20 Na saccharinate
0.10 0.10 0.10 Menthol/peppermint aroma 0.08 0.20 0.15 Ternary
mixture of Aloe 0.02 0.70 0.10 extract, magnesium ascorbyl
phosphate and strawberry leaf extract (quantity ratio: 96.5:3.2:0.3
w/w/w) Bisabolol 0.01 0.05 0.20 Melissa extract (Extrapon 0.30 0.50
0.05 Melissa, Symrise) Sage extract (Extrapon 0.30 0.10 0.05 Sage,
Symrise) Dye 0.01 0.01 0.01 Water, dist. ad 100.00 ad 100.00 ad
100.00
5.7. Mouthwash Concentrate
TABLE-US-00017 [0133] I (%) II (%) III (%) Ethanol, 95% 80.00 80.00
80.00 Na cyclamate 0.15 0.15 0.15 Menthol/aniseed/ 1.50 2.00 2.00
eucalyptol aroma Dye 0.01 0.01 0.01 Ternary mixture of Aloe 1.50
2.50 5.00 extract, sodium ascorbyl phosphate and meadowsweet herb
extract (quantity ratio: 90:9:1 w/w/w) Green tea extract 0.20 1.00
0.50 (Extrapon Green Tea GW, Symrise) Bisabolol 0.50 0.20 1.00
Water, dist. ad 100.00 ad 100.00 ad 100.00
5.8. Chewing Gum
TABLE-US-00018 [0134] I (%) II (%) III (%) Chewing gum base 21.00
21.00 21.00 Glucose syrup 16.50 16.50 16.50 Glycerin 0.50 0.50 0.50
Confectioners' sugar 60.30 60.00 59.80 Menthol/spearmint aroma 1.20
1.00 0.70 Ternary mixture of Aloe 0.50 1.00 1.50 extract, magnesium
ascorbyl phosphate and strawberry leaf extract (quantity ratio:
90:9:1 w/w/w)
5.9. Sugar-Free Chewing Gum
TABLE-US-00019 [0135] I (%) II (%) III (%) Chewing gum base 30.00
30.00 30.00 Sorbitol, powder 38.45 38.40 38.30 Palatinite 9.50 9.50
9.50 Xylitol 2.00 2.00 2.00 Mannitol 3.00 3.00 3.00 Aspartame 0.10
0.10 0.10 Acesulfame .RTM. K 0.10 0.10 0.10 Emulgum/emulsifier 0.30
0.30 0.30 Sorbitol 70%, in water 14.00 14.00 14.00 Glycerin 1.00
1.00 1.00 Menthol/aniseed/ 1.20 0.80 0.60 cinnamon aroma Ternary
mixture of Aloe 0.35 0.80 1.10 extract, sodium ascorbyl phosphate
and raspberry leaf extract (quantity ratio: 96.5:3.2:0.3 w/w/w)
5.10. Gelatine Capsules for Direct Consumption
TABLE-US-00020 [0136] I (%) II (%) III (%) Gelatin shell: Glycerin
2.014 2.014 2.014 Gelatin 240 Bloom 7.91 7.91 7.91 Sucralose 0.065
0.065 0.065 Allura Red 0.006 0.006 0.006 Brilliant blue 0.005 0.005
0.005 Core composition: Vegetable oil triglyceride 80.0 75.0 77.5
(coconut oil fraction) Aroma B 9.95 12.0 12.0 Ternary mixture of
Aloe 0.05 3.0 0.5 extract, magnesium ascorbyl phosphate and
raspberry leaf extract (quantity ratio: 90:9:1 w/w/w)
[0137] Aroma B was of the following composition (values in each
case in wt. %):
0.1% neotame powder, 0.05% aspartame, 29.3% peppermint arvensis
oil, 29.3% peppermint piperita oil Willamette, 2.97% sucralose,
2.28% triacetin, 5.4% diethyl tartrate, 12.1% peppermint oil
yakima, 0.7% ethanol, 3.36% 2-hydroxyethylmenthyl carbonate, 3.0%
2-hydroxypropylmenthyl carbonate, 0.27% vanillin, 5.5% d-limonene,
5.67% L-menthyl acetate.
[0138] The gelatine capsules suitable for direct consumption
(production in a manner similar to WO 2004/050069) had a diameter
of 5 mm, the weight ratio of core material to shell material was
90:10. The capsule opened in the mouth within less than 10 seconds
and dissolved completely within less than 50 seconds.
EXAMPLES 6
Further Formulations Comprising Preparations According to the
Invention with a Collagen Synthesis Stimulating Activity
TABLE-US-00021 [0139] RAW MATERIAL NAME WEIGHT % (MANUFACTURER)
INCI 6.1 6.2 6.3 6.4 6.5 6.6 6.7 6.8 6.9 6.10 Aloe extract 0.9 1.8
0.9 2.0 0.8 1.5 2.7 2.0 0.6 1.0 Sodium ascorbyl 0.09 0.09 0.5 0.15
0.5 0.2 phosphate Magnesium 0.18 0.3 0.27 0.06 ascorbyl phosphate
Raspberry leaf 0.01 0.1 0.1 0.05 0.02 extract Meadowsweet 0.02 0.1
herb extract Strawberry leaf 0.03 0.01 extract Blackberry leaf 0.01
extract -(-Alpha-)- Bisabolol 0.3 0.4 0.3 0.1 0.3 0.2 0.05 0.2 0.5
0.1 Bisabolol, natural (Symrise) Ginger CO.sub.2 Zingiber 0.003
0.004 0.003 0.005 0.003 0.002 0.001 0.002 0.01 0.001 extract
(Flavex) officinale (ginger) root extract Abil 350 Dimethicone 0.5
2.0 1.0 0.5 0.5 (Degussa- Goldschmidt) Allantoin (Merck) Allantoin
0.2 0.1 Aloe Vera Gel Water (aqua), 3.0 3.0 Concentrate 10/1 Aloe
(Symrise) barbadensis leaf juice Alugel 34 TH Aluminium 1.0
(Baerlocher) stearate Aqua-Ceramide Cetyloxypropyl 0.1 0.1 (Kao)
glyceryl methoxypropyl myristamide Arbutin (Sabinsa) .beta.-Arbutin
1.0 Sodium ascorbyl Sodium ascorbyl 2.0 1.0 phosphate (EMD
phosphate Chemicals) Butylene glycol Butylene glycol 5.0 Carbopol
ETD Carbomer 0.2 2050 (Noveon) Carbopol Ultrez-10 Carbomer 0.1
(Noveon) Ceramide 2 Ceramide 2 0.1 (Sederma) Ceramide PC104
Hydroxypropyl 0.1 (Pacific bispalmitamide Corporation) MEA Ceramide
SL Hydroxyethyl 0.1 (Sino Lion) palmityl oxyhydroxy- propyl palmit-
amide Cetiol OE (Cognis) Dicaprylyl ether 4.0 Cetiol SB 45
Butyrospermum 1.0 (Cognis) parkii (shea butter) Citric acid 10%
Citric acid 0.3 sol. Comperlan 100 Cocamide MEA 0.5 (Cognis)
Dihydroxyacetone Dihydroxyacetone 5.0 (Merck) Dow Corning 246
Cyclohexa- 2.0 Fluid (Dow siloxane and Corning) cyclopenta-
siloxane Dow Corning 345 Cyclomethicone 0.5 Fluid (Dow Corning)
D-Panthenol Panthenol 1.0 (BASF) Dracorin CE Glyceryl stearate 5.0
5.0 1.5 (Symrise) citrate Dracorin GMS Glyceryl stearate 2.0 2.0
(Symrise) Dracorin GOC Glyceryl oleate 2.0 (Symrise) citrate,
caprylic/capric triglyceride Drago-Beta- Water (aqua), 0.3 Glucan
(Symrise) butylene glycol, glycerin, Avena sativa (oat), kernel
extract Dragocid Liquid Phenoxyethanol, 0.8 0.7 0.7 0.8 0.8
(Symrise) methylparaben, ethylparaben, butylparaben, propylparaben,
isobutylparaben Dragoderm Glycerin, 2.0 (Symrise) Triticum vulgare
(wheat) gluten, water (aqua) Drago-Oat-Active Water (aqua), 1.0
(Symrise) butylene glycol, Avena sativa (oat) kernel extract
Dragosan W/O Polyglyceryl-3 1.0 Liquid (Symrise) polyricinoleate,
sorbitan isostearate Dragosan W/O P Sorbitan 6.0 (Symrise)
isostearate, hydrogenated castor oil, ceresin, beeswax (cera alba)
Dragoxat EH Ethylhexyl 3.0 3.0 4.0 3.0 (Symrise) ethylhexanoate
Dragoxat 89 Ethylhexyl 2.0 (Symrise) ethylisono- nanoate EDETA B
powder Tetrasodium 0.1 (BASF) EDTA EDETA DB Disodium EDTA 0.1 0.1
(BASF) Emulsiphos Potassium cetyl 2.0 1.5 2.0 (Symrise) phosphate,
hydrogenated palm glycerides Ethanol 96% Ethanol 2.0 30.0 Extrapone
Green Glycerin, water 0.2 Tea GW (Symrise) (aqua), Camellia
sinensis leaf extract Extrapone Witch Propylene 1.0 Hazel
Distillate glycol, colorless Hamamelis (Symrise) virginiana (witch
hazel) water, water (aqua), Hamamelis virginiana (witch hazel)
extract Extrapone Glycerin, water 0.3 0.5 Rosemary GW (aqua),
(Symrise) Rosmarinus officinalis (rosemary) leaf extract Farnesol
Farnesol 0.5 (Symrise) Frescolat ML Menthyl lactate 0.8 cryst.
(Symrise) Genapol LRO Sodium laureth 37.0 liquid (Cognis) sulfate
Givobio GZN Zinc gluconate 0.5 (Seppic) Glycerin 85% Glycerin 3.0
2.0 4.0 4.7 2.0 1.5 3.0 Hydrolite-5 Pentylene glycol 5.0 3.5
(Symrise) Hydroviton Water, glycerin, 1.0 (Symrise) sodium lactate,
TEA lactate, serine, lactic acid, urea, sorbitol, sodium chloride,
lauryl diethylene- diaminoglycine, lauryl amino- propylglycine,
allantoin Irgasan DP 300 Triclosan 0.3 (Ciba Gelgy) Isodragol
Triisononanoin 2.0 3.0 (Symrise) Isopropyl palmitate Isopropyl 4.0
4.0 (Symrise) palmitate Karion F (Merck) Sorbitol 2.0 Keltrol RD
(CP- Xanthan gum 0.2 0.1 Kelco) Keltrol T (Danby- Xanthan gum 0.2
0.3 Chemie) Kojic acid Kojic acid 1.0 (Cosmetochem) Lanette 16
Cetyl alcohol 1.0 1.0 (Cognis) Lanette O Cetearyl alcohol 3.0 1.0
2.0 (Cognis) Lara Care A-200 Galactoarabinan 0.3 (Rahn) Magnesium
Magnesium 0.7 chloride (Merck) chloride Merquat 550
Polyquaternium-7 0.5 (Ondeo Nalco) NaOH 10% sol. Sodium 0.3
hydroxide Naringin (Exquim) 4',5,7-trihydroxy- 0.5 2.0 flavone
7-O-neo- hesperidoside Sodium benzoate Sodium 0.5 benzoate Natrosol
250 HHR Hydroxyethyl- 0.3 (Aqualon) cellulose Neo Heliopan 357
Butyl methoxy- 1.0 (Symrise) dibenzoyl- methane Neo Heliopan AP
Disodium phenyl 10 (Symrise) dibenzimidazole (10% as sodium
tetrasulfonate salt) Neo Heliopan AV Ethylhexyl 3.0 (Symrise)
methoxy- cinnamate Neo Heliopan Phenylbenz- 6.7 Hydro (Symrise)
imidazole sulfonic acid (15% as sodium salt) Neo Heliopan
4-Methylbenzyl- 1.5 MBC (Symrise) idene camphor Neo Heliopan OS
Ethylhexyl 5.0 (Symrise) salicylate Neutral oil Caprylic/capric 6.0
4.0 2.0 6.0 10.0 triglyceride Oxynex 2004 BHT 0.1 (Merck) Paraffin
oil 5 E Paraffinum 4.0 (Parafluid) liquidum PCL Liquid 100 Cetearyl
3.0 5.0 7.0 (Symrise) ethylhexoate PCL Solid Stearyl 2.0 (Symrise)
heptanoate, stearyl caprylate PCL Liquid Cetearyl 12.0 3.0
(Symrise) ethylhexanoate, isopropyl myristate Pemulen TR-2
Acrylates/C10-30 0.3 0.2 (Noveon) alkyl acrylate crosspolymer
4-(1-Phenylethyl)- 4-(1-Phenyl- 0.5 1,3-benzenediol ethyl)-1,3-
benzenediol 1,2-Propylene Propylene glycol 5.0 glycol 99P GC
Pseudoceramide N-(1-hexa- 0.1 0.2 0.5 391 decanol)-4-
hydroxy-L-
proline (1- hexadecyl ester) Retinyl palmitate Retinyl palmitate
0.2 in oil (DSM Nutritional Products) Sepigel 305 Polyacrylamide,
1.0 C13-14 isoparaffin, laureth-7 Sodium chloride Sodium chloride
1.0 Sodium hydroxide Sodium 0.3 0.6 0.4 (10% sol.) hydroxide
Solubilizer 611674 PEG-40 2.0 (Symrise) hydrogenated castor oil,
trideceth-9, water (aqua) Sunflower oil Helianthus 5.0 (Wagner)
annuus (sunflower) seed oil Sweet almond oil Prunus dulcis 5.0
(Wagner) Symdiol 66 1,2-Hexanediol, 0.5 (Symrise) caprylyl glycol
Symrise Fragrance 0.3 0.3 0.3 0.2 0.4 0.4 0.5 0.3 0.3 1.0 Fragrance
Tamasterol (Tama Phytosterols 0.3 Biochemicals) Tego Betaine L7
Cocamidopropyl 6.0 (Degussa) betaine Tegosoft PC 31 0.3 (Degussa)
Tegosoft TN C12-15 alkyl 5.0 5.0 (Degussa) benzoate
Triethanolamine, Triethanolamine 0.5 99% Tocopherol Tocopheryl 0.5
0.5 3.0 0.3 acetate (DSM acetate Nutritional Products) Zirkonal L
450 Aluminium 37.0 (BK Giulini) zirconium pentachloro- hydrate (40%
aqueous solution) Water, Water (aqua) ad 100 ad 100 ad 100 ad 100
ad 100 ad 100 ad 100 ad 100 ad 100 ad 100 demineralized Key to the
following table 6.1 = Skin-lightening O/W day cream 6.2 =
Skin-soothing O/W lotion with plant extracts 6.3 = Aftersun balm
6.4 = Body spray 6.5 = Sunscreen lotion (O/W), broadband protection
6.6 = W/O night cream 6.7 = Shampoo 6.8 = Self-tanning cream 6.9 =
O/W barrier repair cream 6.10 = Antiperspirant/deodorant
roll-on
* * * * *